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Serotoninergic Neurons and 5-HT Receptors in the CNS pp 409–438Cite as

Neuropharmacology of 5-HT3 Receptor Ligands

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Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 129))

Abstract

Gaddum and Picarelli(1957), using the guinea pig ileum, were the first researchers to show that 5-hydroxytryptamine (5-HT) can mediate a neuronal depolarising response and release of acetylcholine. A clarification of the nature and function of the receptor mediating the response to 5-HT has subsequently taken some 40 years. The present chapter reviews the beginnings of a pharmacological understanding of this receptor and the therapeutic implications of drugs which have affinity for it.

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References

  • Abuzzahab FS (1991) Ondansetron: a novel anti-anxiety agent. In: Briley M, File SE (eds) New concepts in anxiety. MacMillan, Basingstoke, pp 185–189

    Google Scholar 

  • Alhaider AA, Lei SZ, Wilcox GL (1991) Spinal 5-HT3 receptor-mediated anti-nociception: possible release of GABA. J Neurosci 11:1881–1887

    PubMed  CAS  Google Scholar 

  • Andrews PLR (1994) 5-HT3 receptor antagonists and antiemesis. In: King FD, Jones BJ, Sanger GJ (eds) 5-Hydroxytryptamine-3 receptor antagonists. CRC, Boca Raton, pp 255–317

    Google Scholar 

  • Andrews N, File SE (1993) Handling history of rats modifies behavioural effects of drugs in the elevated plus-maze test of anxiety. Eur J Pharmacol 235:109–112

    Article  PubMed  CAS  Google Scholar 

  • Andrews PA, Quan V, Ogg CS (1995) Ondansetron for symptomatic relief in terminal uraemia. Nephrol Dial Transplant 10: 140

    PubMed  CAS  Google Scholar 

  • Ashby CR, Minabe Y, Edwards E, Wang RY (1991) 5-HT3-like receptors in the rat medial prefrontal cortex: an electrophysiological study. Brain Res 550:181–191

    Article  PubMed  CAS  Google Scholar 

  • Ashby CR, Edwards E, Wang RY (1992) Action of serotonin in the medial prefrontal cortex: mediation by serotonin3-like receptors. Synapse 10:7–15

    Article  PubMed  CAS  Google Scholar 

  • Azami J, Fozard JR, Round AA, Wallis DI (1985) The depolarising action of 5-hydroxytryptamine on rabbit vagal primary afferent and sympathetic neurones and its selective blockade by MDL 72222. Naunyn Schmiedebergs Arch Pharmacol 328:762–763

    Article  Google Scholar 

  • Bailey J, Potokar J, Nutt D (1994) Can the GI disturbance produced by the SSRIs be attenuated by a 5-HT3 antagonist? Neuropsychopharmacology 10:220

    Google Scholar 

  • Barnes JM, Barnes NM, Costall B, Naylor RJ, Tyers MB (1989) 5-HT3 receptors mediate inhibition of acetylcholine release in cortical tissue. Nature 338:762–763

    Article  PubMed  CAS  Google Scholar 

  • Barnes JM, Costall B, Coughlan J, Domeney AM, Gerrard PA, Kelly ME, Naylor RJ, Onaivi ES, Tomkins DM, Tyers MB (1990a) The effects of ondansetron, a 5-HT3 receptor antagonist, on cognition in rodents and primates. Pharmacol Biochem Behav 35:955–962

    Article  PubMed  CAS  Google Scholar 

  • Barnes NM, Costall B, Naylor RJ (1988) [3H]Zacopride: ligand for the identification of 5-HT3 recognition sites. J Pharm Pharmacol 40:548–551

    Article  PubMed  CAS  Google Scholar 

  • Barnes NM, Costall B, Naylor RJ, Williams TJ, Wischik CM (1990b) Normal densities of 5-HT3 receptor recognition sites in Alzheimer’s disease. Neuroreport 1:253–254

    Article  PubMed  CAS  Google Scholar 

  • Barrat JE, Gleeson S (1991) Anxiolytic effects of 5-HT1A agonists, 5-HT3 antagonists and benzodiazepines: conflict and drug discrimination studies. In: Rogers RJ, Cooper SJ (eds) 5-HT1A agonists, 5-HT3 antagonists and benzodiazepines, their comparative behavioural pharmacology. Wiley, Chichester, pp 59–105

    Google Scholar 

  • Belelli D, Balcarek JM, Hope AG, Peters JA, Lambert JT, Blackburn TP (1995a) Cloning and functional expression of a human 5-hydroxytryptamine type 3As receptor (5-HT3R-As) subunit. Mol Pharmacol 48:1054–1062

    PubMed  CAS  Google Scholar 

  • Belelli D, Hope AG, Peters JA, Lambert JL, Blackburn TP, Balcarek JM (1995b) Functional properties of a human recombinant 5-HT3 receptor expressed in Xenopus laevis oocytes. Br J Pharmacol 116:229P

    Google Scholar 

  • Bianchi C, Siniscalchi A, Beani L (1990) 5-HT1A agonists increase and 5-HT3 agonists decrease acetylcholine efflux from the cerebral cortex of freely-moving guinea pigs. Br J Pharmacol 101:448–452

    Article  PubMed  CAS  Google Scholar 

  • Blandina P, Goldfarb J, Green JP (1988) Activation of 5-HT3 receptor releases dopamine from rat striatal slice. Eur J Pharmacol 155:349–350

    Article  PubMed  CAS  Google Scholar 

  • Blandina P, Goldfarb J, Walcott J, Green JP (1991) Serotonergic modulation of the release of endogenous norepinephrine from rat hypothalamic slices. J Pharmacol Exp Ther 256:341–347

    PubMed  CAS  Google Scholar 

  • Boess FG, Martin IL (1994) Molecular biology of 5-HT receptors. Neuropharmacology 33:275–317

    Article  PubMed  CAS  Google Scholar 

  • Boess FG, Lummus SCR, Martin IL (1992) Molecular properties of 5-hydroxytryptamine3 receptor type binding sites purified from NG108-15 cells. J Neurochem 59:1692–1701

    Article  PubMed  CAS  Google Scholar 

  • Bolanos FJ, Schechter LE, Miguel MC, Emerit MB, Rumigny JF, Hamon M, Gozlan H (1990) Common pharmacological and physiological properties of 5-HT3 binding sites in the rat cerebral cortex and NG108-15 clonal cells. Biochem Pharmacol 40:1541–1550

    Article  PubMed  CAS  Google Scholar 

  • Bradley PB, Engel G, Feniuk W, Fozard JR, Humphrey PPA, Middlemiss DN, Mylecharane EJ, Richardson BP, Saxena PR (1986) Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine. Neuropharmacology 25:563–576

    Article  PubMed  CAS  Google Scholar 

  • Bratt AM, Kelly ME, Domeney AM, Naylor RJ, Costall B (1994) Failure of ondansetron to attenuate a scopolamine-induced deficit in a stone maze task. Neuroreport 5:1921–1924

    Article  PubMed  CAS  Google Scholar 

  • Brett RR, Prat JA (1990) Chronic handling modifies the anxiolytic effect of diazepam in the elevated plus-maze. Eur J Pharmacol 178:135–138

    Article  PubMed  CAS  Google Scholar 

  • Broggi U, Dones I, Servello D, Ferrazza C (1996) A possible pharmacological treatment of baclofen overdosage. Italian J Neurol Sci 17:179–180

    Article  CAS  Google Scholar 

  • Butcher ME (1993) Global experience with ondansetron and future potential. Oncology 50:191–197

    Article  PubMed  CAS  Google Scholar 

  • Butler A, Hill JM, Ireland SJ, Jordan CC, Tyers MB (1988) Pharmacological properties of GR38032F, a novel antagonist at 5-HT3 receptors. Br J Pharmacol 94:397–412

    Article  PubMed  CAS  Google Scholar 

  • Butler A, Elswood CJ, Burridge J, Ireland SJ, Bunce KT, Kilpatrick GJ, Tyers MB (1990) The pharmacological characterisation of 5-HT3 receptors in three isolated preparations derived from guinea-pig tissues. Br J Pharmacol 101:591–598

    Article  PubMed  CAS  Google Scholar 

  • Carboni E, Acquas E, Leone P, Perrezzani L, Di Chiara G (1988) 5-HT3 receptor antagonists block morphine and nicotine induced place preference conditioning. Eur J Pharmacol 151:1590–160

    Article  Google Scholar 

  • Carey GJ, Costall B, Domeney AM, Gerrard PA, Jones DNC, Naylor RJ, Tyers MB (1992) Ondansetron and arecoline prevent scopolamine-induced cognitive deficits in the marmoset. Pharmacol Biochem Behav 42:75–83

    Article  PubMed  CAS  Google Scholar 

  • Champaneria S, Costall B, Naylor RJ, Robertson DW (1992) Identification and distribution of 5-HT3 recognition sites in the rat gastrointestinal tract. Br J Pharmacol 106:693–696

    Article  PubMed  CAS  Google Scholar 

  • Chen J, Van Praag HM, Gardner EL (1991) Activation of 5-HT3 receptor by 1-phenylbiguanide increases dopamine release in the rat nucleus accumbens. Brain Res 543:354–357

    Article  PubMed  CAS  Google Scholar 

  • Cheng CHK, Costall B, Kelly ME, Naylor RJ (1994) Actions of 5-hydroxytryptophan to inhibit and disinhibit mouse behaviour in the light dark test. Eur J Pharmacol 255:39–49

    Article  PubMed  CAS  Google Scholar 

  • Chopin P, Briley M (1987) Animal models of anxiety: the effect of compounds that modify 5-HT neurotransmission. Trends Pharmacol Sci 8:383–388

    Article  CAS  Google Scholar 

  • Chugh Y, Saha N, Sankaranarayanan A, Sharma PL (1991a) Memory enhancing effects of granisetron (BRL 43694) in a passive avoidance task. Eur J Pharmacol 203:121–123

    Article  PubMed  CAS  Google Scholar 

  • Chugh Y, Saha N, Sankaranarayanan A, Datta H (1991b) Enhancement of memory retrieval and attenuation of scopolamine induced amnesia following administration of 5-HT3 antagonist ICS205-930. Pharmacol Toxicol 69:105–106

    Article  PubMed  CAS  Google Scholar 

  • Consolo S, Bertorelli R, Russi G, Zambelli M, Ladinsky H (1994) Serotonergic facilitation of acetylcholine release in vivo from rat dorsal hippocampus via serotonin 5-HT3 receptors. J Neurochem 62:2254–2261

    Article  PubMed  CAS  Google Scholar 

  • Costall B, Naylor RJ (1991) Anxiolytic effects of 5-HT3 antagonists in animals. In: Rodgers RJ, Cooper SJ (eds) 5-HT1A agonists, 5-HT3 antagonists and benzodiazepines, their comparative behavioural pharmacology. Wiley, Chichester, pp 133–157

    Google Scholar 

  • Costall B, Naylor RJ (1994a) 5-HT3 receptor antagonism and schizophrenia. In: King FD, Jones BJ, Sanger GJ (eds) 5-Hydroxytryptamine-3 receptor antagonists. CRC, Boca Raton, pp 183–219

    Google Scholar 

  • Costall B, Naylor RJ (1994b) 5-HT3 receptor antagonists in the treatment of cognitive disorders. In: King FD, Jones BJ, Sanger GJ (eds) 5-Hydroxytryptamine-3 receptor antagonists. CRC, Boca Raton, pp 203–219

    Google Scholar 

  • Costall B, Domeney AM, Naylor RJ (1986) 5-Hydroxytryptamine M-receptor antagonism to prevent cisplatin-induced emesis. Neuropharmacology 25:959–961

    Article  PubMed  CAS  Google Scholar 

  • Costall B, Domeney AM, Naylor RJ, Tyers MB (1987) Effects of the 5-HT3 receptor antagonist GR38032F, on raised dopaminergic activity in the mesolimbic system of the rat and marmoset brain. Br J Pharmacol 92:881–894

    Article  PubMed  CAS  Google Scholar 

  • Costall B, Kelly ME, Naylor RJ, Onaivi ES, Tyers MB (1989) Neuroanatomical sites of action of 5-HT3 receptor agonist and antagonists for alteration of aversive behaviour in the mouse. Br J Pharmacol 96:325–332

    Article  PubMed  CAS  Google Scholar 

  • Costall B, Naylor RJ, Tyers MB (1990) The psychopharmacology of 5-HT3 receptors. Pharmacol Ther 47:181–202

    Article  PubMed  CAS  Google Scholar 

  • Couturier EGM, Hering R, Foster CA, Steiner TJ, Rose FC (1991) First clinical study of the selective 5-HT3 antagonist, granisetron (BRL43694), in the acute treatment of migraine headache. Headache 31:296–297

    Article  PubMed  CAS  Google Scholar 

  • Crook TH, Lakin M (1991) Effects of ondansetron image-associated memory impairment. Proceedings of the 5th world congress of biological psychiatry, Florence

    Google Scholar 

  • Cubeddu LX, Hoffman IS, Fuenmayor NT, Malave JJ (1992) Changes in serotonin metabolism in cancer patients: its relationship to nausea and vomiting induced by chemotherapeutic agents. Br J Cancer 66:198–203

    Article  PubMed  CAS  Google Scholar 

  • Cunningham D, Turner A, Hawthorn J, Rosin RD (1989) Ondansetron with and without dexamethasone to treate chemotherapy. Lancet 1:1323

    Article  PubMed  CAS  Google Scholar 

  • Dershwitz M, Rosow S-E, Dibiase PM, Joslyn AF, Sanderson PE (1992) Ondansetron is effective in decreasing postoperative nausea and vomiting. Clin Pharmacol Ther 52:96–101

    Article  PubMed  CAS  Google Scholar 

  • Domeney AM, Costall B, Gerrard PA, Jones DN, Naylor RJ, Tyers MD (1991) The effect of ondansetron on cognitive performance in the marmoset. Pharmacol Biochem Behav 38:169–175

    Article  PubMed  CAS  Google Scholar 

  • Donatsch P, Engel G, Richardson BP, Stadler P (1984) ICS205–930:a highly selective and potent antagonist at peripheral neuronal 5-hydroxytryptamine (5-HT) receptors. Br J Pharmacol 81:34P

    Google Scholar 

  • Doty P, Zacny JP, de Wit H (1994) Effects of ondansetron pretreatment on acute responses to ethanol in social drinkers. Behav Pharmacol 5:461–469

    Article  PubMed  CAS  Google Scholar 

  • Downie DL, Hope AG, Lambert JJ, Peters JA, Blackburn TP, Jones BJ (1994) Pharmacological characterisation of the apparent splice variants of the murine 5-HT3 R-A subunit expressed in Xenopus laevis oocytes. Neuropharmacology 33:473–482

    Article  PubMed  CAS  Google Scholar 

  • Dunn RW, Carlezon WA, Corbett R (1991) Preclinical anxiolytic versus antipsychotic profiles of the 5-HT3 antagonists ondansetron, zacopride, 3-tropanyl-1H-indole-3-carboxylic acid ester, and 1-H, 3, 5H-tropan-3-yl-3,5-dichlorobenzoate. Drug Dev Res 23:289–300

    Article  CAS  Google Scholar 

  • Edwards E, Harkins KL, Ashby CR, Wang RY (1991) The effects of 5-HT3 receptor agonists on phosphoinositide hydrolysis in the rat frontocingulate and entorhinal cortices. J Pharmacol Exp Ther 256:1025–1032

    PubMed  CAS  Google Scholar 

  • Elliott P, Wallis DI (1988) The depolarising action of 5-hydroxtryptamine on rabbit isolated preganglionic cervical sympathetic nerves. Naunyn Schmiedebergs Arch Pharmacol 338:608–615

    Article  PubMed  CAS  Google Scholar 

  • Elliott P, Seemungal BM, Wallis DI (1990) Antagonism of the effects of 5-hydroxytryptamine on the rabbit isolated vagus nerve by BRL43694 and metoclopramide. Naunyn Schmiedbergs Arch Pharmacol 341:503–509

    CAS  Google Scholar 

  • Eschalier A, Kayser V, Guilband G (1989) Influence of a specific 5-HT3 antagonist on carrageenan-induced hyperalgesia in rats. Pain 36:249–255

    Article  PubMed  CAS  Google Scholar 

  • Evans JE (1993) Nausea, abdominal pain and diarrhoea of uncertain cause responding to ondansetron. Med J Aust 159:125–127

    PubMed  CAS  Google Scholar 

  • Ferrari MD, Wilkinson M, Hirt D, Lataste X, Notter M (1991) Efficacy of ICS205-930 a novel 5-hydroxytryptamine-3 5-HT3 receptor antagonist in the prevention of migraine attacks: a complex answer to a simple question. Pain 45:283–291

    Article  PubMed  CAS  Google Scholar 

  • File SE, Andrews N, Wu PY, Zharkovsky A, Zangrossi H (1992) Modification of chlordiazepoxide’s behavioural and neurochemical effects by handling and plus-maze experience. Eur J Pharmacol 218:9–14

    Article  PubMed  CAS  Google Scholar 

  • Fortune DH, Ireland SJ, Tyers MB (1983) Phenylbiguanide mimics the effects of 5-hydroxytryptamine on the rat isolated vagus nerve and superior cervical ganglion. Br J Pharmacol 79:298P

    Google Scholar 

  • Fozard JR (1983) Differences between receptors for 5-hydroxytryptamine on autonomic neurones revealed by nor-(—)cocaine. J Auton Pharmacol 3:21–216

    Article  PubMed  CAS  Google Scholar 

  • Fozard JR (1984a) MDL72222: a potent and highly selective antagonist at neuronal 5-hydroxytryptamine receptors. Naunyn Schmiedebergs Arch Pharmacol 326:36–44

    Article  PubMed  CAS  Google Scholar 

  • Fozard JR (1984b) Neuronal 5-HT receptors in the periphery. Neuropharmacology 23:1473–1486

    Article  PubMed  CAS  Google Scholar 

  • Fozard JR (1984c) 5-Hydroxytryptamine in the pathophysiology of migraine. In: Bevan JA, Godfraind T, Maxwell RA, Stoclet JC, Worcel M (eds) Vascular neuroeffector mechanisms. Elsevier, Amsterdam, pp 321–329

    Google Scholar 

  • Fozard JR (1989) The development and early clinical evaluation of selective 5-HT3 receptor antagonists. In: Fozard JR (ed) The peripheral actions of 5-hydroxytryptamine. Oxford University Press, New York, pp 354–376

    Google Scholar 

  • Fozard JR (1994) Role of 5-HT3 receptors in nociception. In: King FD, Jones BJ, Sanger GJ (eds) 5-Hydroxytryptamine3 receptor antagonists. CRC, Boca Raton, pp 241–253

    Google Scholar 

  • Fozard JR, Gittos MW (1983) Selective blockade of 5-hydroxytryptamine neuronal receptors by benzoic acid esters of tropine. Br J Pharmacol 80:511P

    Article  Google Scholar 

  • Fozard JR, Loisy C, Tell GP (1985) Blockade of neuronal 5-hydroxytryptamine receptors with MDL72222: a novel approach to the symptomatic treatment of migraine. In: Rose FC (ed) Migraine clinical and research advances. Skarger, Basle, pp 264–272

    Google Scholar 

  • Fozard JR, Mobarok Ali ATM (1978) Blockade of neuronal tryptamine receptors by metoclopramide. Eur J Pharmacol 49:109–112

    Article  PubMed  CAS  Google Scholar 

  • Gaddum JHR, Picarelli ZP (1957) Two kinds of tryptamine receptor. Br J Pharmacol 12:323–328

    CAS  Google Scholar 

  • Galzin AM, Poncet V, Langer SZ (1990) 5-HT3 receptor agonists enhance the electrically evoked release of [3H]5-HT in guinea-pig frontal cortex slices. Br J Pharmacol 100:307P

    Google Scholar 

  • Gehlert DR, Gackenheimer SL, Wong DT, Robertson DW (1991) Localisation of 5-HT3 receptors in the rat brain using [3H]LY 278584. Brain Res 553:149–154

    Article  PubMed  CAS  Google Scholar 

  • Gill CH, Peters JA, Lambert JJ (1995) An electrophysiological investigation of the properties of a murine recombinant 5-HT3 receptor stably expressed in HEK293 cells. Br J Pharmacol 114:1211–1221

    Article  PubMed  CAS  Google Scholar 

  • Giordano J (1991) Analgesic profile of centrally administered 2-methylserotonin against acute pain in rats. Eur J Pharmacol 199:233–236

    Article  PubMed  CAS  Google Scholar 

  • Giordani J, Dyche J (1989) Differential analgesic actions of serotonin 5-HT3 receptor antagonists in the mouse. Neuropharmacology 28:423–427

    Article  Google Scholar 

  • Giordani J, Rogers L (1989) Peripherally administered serotonin 5-HT3 receptor antagonists reduce inflammatory pain. Eur J Pharmacol 170:83–86

    Article  Google Scholar 

  • Glaum SR, Proudfit HK, Anderson EG (1988) Reversal of the antinociceptive effects of intrathecally administered serotonin in the rat by a selective 5-HT3 receptor antagonist. Neurosci Lett 95:313–317

    Article  PubMed  CAS  Google Scholar 

  • Glaum SR, Proudfit HK, Anderson EG (1990) 5-HT3 receptors modulate spinal nociceptive reflexes. Brain Res 510:12–18

    Article  PubMed  CAS  Google Scholar 

  • Gompels M, McWilliams S, O’Hare M, Harris JR, Pinching FJ, Main J (1993) Ondansetron usage in HIV positive patients — a pilot study on the control of nausea and vomiting in paitents on high dose co-trimoxazole for Pneumocytis carinii pneumonia. Int J Std Aids 4: 293–296

    PubMed  CAS  Google Scholar 

  • Greenshaw AJ (1992) Differential effects of antipsychotics and the 5-HT3 antagonist ondansetron on electrical self-stimulation of the VTA in rats. Clin Neuropsychopharmacol 15:88–92

    Article  Google Scholar 

  • Guikontes E, Spantideas A, Diakakis J (1992) Ondansetron and hyperemesis gravidarum. Lancet 340:1223

    Article  PubMed  CAS  Google Scholar 

  • Hagan RM, Butler A, Hill JM, Jordan CC, Ireland SJ, Tyers MB (1987) Effect of the 5-HT3 receptor antagonist GR38032F on responses to injection of a neurokinin agonist into the ventral tegmental area of the rat brain. Eur J Pharmacol 138:303–305

    Article  PubMed  CAS  Google Scholar 

  • Hagan RM, Oakley NR, Burridge J, Kilpatrick GJ, Tyers MB (1991) Effects of the 5-HT3 receptor antagonist, GR68755, in models of anxiety and raised mesolimbic dopaminergic activity in the rat. Proceedings of the international meeting on serotonin, Birmingham, p 115

    Google Scholar 

  • Herberg LJ, De Belleroche JS, Rose IC, Montgomer AMJ (1992) Effect of the 5-HT3 receptor antagonist ondansetron on hypothalamic self-stimulation in rats and its interaction with the CCK analogue caerulin. Neurosci Lett 140:16–18

    Article  PubMed  CAS  Google Scholar 

  • Hertling-Jaweed S, Bandini G, Hucho F (1990) Purification of nicotinic receptors. In: Hulme EC (ed) Receptor biochemistry, a practical approach. IRL Press, London, pp 163–176

    Google Scholar 

  • Higashi H, Nishi S (1982) 5-Hydroxytryptamine receptors on visceral primary afferent neurones of rabbit nodose ganglia. J Physiol (Lond) 323:543–567

    PubMed  CAS  Google Scholar 

  • Higgins GA, Jones BJ, Oakley NR, Tyers MB (1991) Evidence that the amygdala is involved in the disinhibitory effects of 5-HT3 receptor antagonists. Psychopharmacology 104:545–551

    Article  PubMed  CAS  Google Scholar 

  • Higgins GA, Joharchi N, Nguyen P, Sellers EM (1992) Effect of the 5-HT3 receptor antagonists, MDL72222 and ondansetron on morphine place conditioning. Psychopharmacology 106:315–320

    Article  PubMed  CAS  Google Scholar 

  • Hoagland AC, Bennet JM, Morrow GR, Carnrike CLM (1983) Oncologist’s view of cancer patients’ non-compliance. Am J Oncol 6: 239–244

    Article  CAS  Google Scholar 

  • Holtum JR, Gershon S (1992) The cholinergic model of dementia, Alzheimer type: progression from the unitary transmitter concept. Dementia 3:174–185

    Google Scholar 

  • Hope AG, Downie DL, Sutherland L, Lambert JL, Peters JA, Burchell B (1993) Cloning and functional expression of an apparent splice variant of the murine 5-HT3 receptor A subunit. Eur J Pharmacol 245:187–192

    Article  PubMed  CAS  Google Scholar 

  • Hope AG, Brown AM, Peters JA, Lambert JJ, Balcarek JM, Blackburn TP (1995) Characterisation of a cloned human 5-HT3 receptor subunit stably expressed in HEK293 cells. Br J Pharmacol 116:82P

    Google Scholar 

  • Hoyer D, Neijt HC (1988a) Identification of serotonin 5-HT3 recognition sites by radioligand binding in NG108-15 neuroblastoma-glioma cells. Eur J Pharmacol 143:291–292

    Article  Google Scholar 

  • Hoyer D, Neijt HC (1988b) Identification of serotonin 5-HT3 recognition sites in membranes of N1E-115 neuroblastoma cells by radioligand binding. Mol Pharmacol 33:303–309

    PubMed  CAS  Google Scholar 

  • Hoyer D, Waeber C, Karpf A, Neijt H, Palacios JM (1989) [3H]CS205-930 labels 5-HT3 recognition sites in membranes of cat and rabbit vagus nerve and superior cervical ganglion. Naunyn Schmiedebergs Arch Pharmacol 340:396–402

    Article  PubMed  CAS  Google Scholar 

  • Imoto K, Busch C, Sakmann B, Mishina M, Konno T, Nakai J, Bujo H, Mori Y, Fukuda K, Numa S (1988) Rings of negatively charged amino acids determine the acetylcholine receptor channel conductance. Nature 335:645–648

    Article  PubMed  CAS  Google Scholar 

  • Imperato A, Angelucci L (1989) 5-HT3 receptor controls dopamine release in nucleus accumbens of freely moving rats. Neurosci Lett 101:214–217

    Article  PubMed  CAS  Google Scholar 

  • Imperato A, Puglisi-Allergra S, Zocchi A, Scrocco MG, Casolini P, Angelucci L (1990) Stress activation of limbic and cortical dopamine release is prevented by ICS205-930 but not diazepam. Eur J Pharmacol 175:211–214

    Article  PubMed  CAS  Google Scholar 

  • Ireland SJ, Tyers MB (1987) Pharmacological characterisation of 5-hydroxytryptamine induced depolarisations of the rat isolated vagus nerve. Br J Pharmacol 90:229–238

    Article  PubMed  CAS  Google Scholar 

  • Ireland SJ, Straughan DW, Tyers MB (1987) Influence of 5-hydroxytryptamine uptake on the apparent 5-hydroxytryptamine antagonist potency of metoclopramide in the rat isolated superior cervical ganglion. Br J Pharmacol 90:151–160

    Article  PubMed  CAS  Google Scholar 

  • Iversen SD (1984) 5-HT and anxiety. Neuropharmacology 23:1553–1560

    Article  PubMed  CAS  Google Scholar 

  • Jiang LH, Ashby CR, Kasser RJ, Wang RY (1990) The effect of intraventricular administration of the 5-HT3 receptor agonist 2-methylserotonin on the release of dopamine in the nucleus accumbens: an in vivo chronocoulometric study. Brain Res 513:156–160

    Article  PubMed  CAS  Google Scholar 

  • Jakala P, Sirvio J, Riekkinen PJ (1993) The effects of tacrine and zacopride on the performance of adult rats in the working memory task. Gen Pharmacol 24:675–679

    Article  PubMed  CAS  Google Scholar 

  • Johnson BA, Cowen PJ (1993) Alcohol-induced reinforcement: dopamine and 5-HT3 receptor interactions in animals and humans. Drug Dev Res 30:153–169

    Article  CAS  Google Scholar 

  • Johnson DS, Heinemann SF (1992) Cloning and expression of the rat 5-HT3 receptor reveals species-specific sensitivity to curare antagonism. Soc Neurosci Abstr 18:249

    Google Scholar 

  • Johnson DS, Heinemann SF (1993) Rat 5-HT3 receptor expression in the central and peripheral nervous system — an in situ hybridization study. Soc Neurosci Abstr 19:632

    Google Scholar 

  • Johnson RM, Inouye GT, Eglen RM, Wong EH (1993) 5-HT3 receptor ligands lack modulatory influence on acetylcholine release in rat entorhinal cortex. Naunyn Schmiedebergs Arch Pharmacol 347:241–247

    Article  PubMed  CAS  Google Scholar 

  • Johnston AL, File SE (1984) 5-HT and anxiety: promises and pitfalls. Pharmacol Biochem Behav 24:1467–1470

    Article  Google Scholar 

  • Jones BJ, Piper DC (1994) 5-HT3 receptor antagonists in anxiety. In: King FD, Jones BJ, Sanger GJ (eds) 5-Hydroxytryptamine-3 receptor antagonists. CRC, Boca Raton, pp 155–181

    Google Scholar 

  • Jones BJ, Costall B, Domeney AM, Kelly ME, Naylor RJ, Oakley NR, Tyers MB (1988) The potential anxiolytic activity of GR38032F, a 5-HT3 receptor antagonist. Br J Pharmacol 93:985–993

    Article  PubMed  CAS  Google Scholar 

  • Keele CA, Armstrong D (1964) Substances producing pain and itch. Williams and Wilkins, Baltimore, pp 152–167

    Google Scholar 

  • Kennett GA, Blackburn TP (1990) Anxiolytic-like actions of BRL 46470, a novel 5-HT3 antagonist. Proceedings of the British Association for Psychopharmacology, annual meeting, Cambridge, England, 17th July, abstract 117

    Google Scholar 

  • Kennett GA, Whitton P, Shah K, Curzon G (1989) Anxiogenic-like effects of mCPP and TFMPP in animal models are opposed by 5-HT1C receptor antagonists. Eur J Pharmacol 164:445–454

    Article  PubMed  CAS  Google Scholar 

  • Kilpatrick GJ, Tyers MB (1992) Interspecies variants of the 5-HT3 receptor. Biochem Soc Trans 20:118–121

    PubMed  CAS  Google Scholar 

  • Kilpatrick GJ, Jones BJ, Tyers MB (1987) Identification and distribution of 5-HT3 receptors in rat brain using radioligand binding. Nature 330:746–748

    Article  PubMed  CAS  Google Scholar 

  • Kilpatrick GJ, Jones B J, Tyers MB (1988) The distribution of specific binding of the 5-HT3 receptor ligand [3H]GR65650 in rat brain using quantitative autoradiography. Neurosci Lett 94:156–160

    Article  PubMed  CAS  Google Scholar 

  • Kilpatrick GJ, Butler A, Burridge J, Oxford AW (1990a) l-(m-Chlorophenyl)-biguanide, a potent high affinity 5-HT3 receptor agonist. Eur J Pharmacol 182:193–197

    Article  PubMed  CAS  Google Scholar 

  • Kilpatrick GJ, Butler A, Hagan RM, Jones BJ, Tyers MB (1990b) [3H]GR67330, a very high affinity ligand for 5-HT, receptors. Naunyn Schmiedebergs Arch Pharmacol 342:22–30

    Article  PubMed  CAS  Google Scholar 

  • Kilpatrick GJ, Barnes NM, Cheng CHK, Costall B, Naylor RJ, Tyers MB (1991) The pharmacological characterisation of 5-HT3 receptor binding sites in rabbit ileum: comparison with those in rat ileum and rat brain. Neurochem Int 19:389–396

    Article  CAS  Google Scholar 

  • King GR, Xue Z, Calvi C, Ellinwood EH (1995) 5-HT3 agonist-induced dopamine overflow during withdrawal from continuous or intermittent cocaine administration. Psychopharmacology (Berl) 117: 458–465

    Article  PubMed  CAS  Google Scholar 

  • Kleinerman KB, Deppe SA, Sargent AI (1993) Use of ondansetron for control of projectile vomiting in patients with neurosurgical trauma: two case reports. Ann Pharmacother 27: 566–568

    PubMed  CAS  Google Scholar 

  • Koch KL, Bingaman S (1993) Effects of ondansetron on morphine-induced nausea, vasopressin and gastric myoelectrical activity in healthy humans. Gastroenterology 104:A535

    Google Scholar 

  • Konno T, Busch C, von Kitzing E, Imoto K, Wang F, Nakai J, Mishina M, Numa S, Sakmann B (1991) Rings of anionic amino acids as structural determinants of ion selectivity in the acetylcholine receptor channel. Proc R Soc Lond B 244:67–79

    Article  Google Scholar 

  • Lader MH (1991) Ondansetron in the treatment of anxiety. In: Racagni G, Brunello N, Fukuda T (eds) Biological psychiatry. Excerpta Medica, Amsterdam, pp 885–887

    Google Scholar 

  • Lambert JJ, Peters JA, Hales TG, Dempster J (1989) The properties of 5-HT3 receptors in clonal cell lines studied by patch-clamp techniques. Br J Pharmacol 97:27–40

    Article  PubMed  CAS  Google Scholar 

  • Lane JD, Pickering CL, Hooper ML, Fagan K, Tyers MB, Emmett-Oglesby MW (1992) Failure of ondansetron to block the discriminative or reinforcing stimulus properties of cocaine in the rat. Drug Alcohol Depend 30:151–162

    Article  PubMed  CAS  Google Scholar 

  • Larijani GE, Gratz I, Afshar M, Minassian S (1991) Treatment of postoperative nausea and vomiting with ondansetron — a randomised, double-blind comparison with placebo. Anaesth Analg 73:246–249

    Article  CAS  Google Scholar 

  • Lazlo J, Lucas VSJ (1981) Emesis as a critical problem in chemotherapy. N Engl J Med 305: 948–949

    Article  Google Scholar 

  • Lecrubier Y, Puech AJ, Azcona A (1991) 5-HT3 receptors in anxiety disorders. Proceedings of the British Association for Psychopharmacology, annual meeting, Cambridge, England, 17th July

    Google Scholar 

  • Leibundgut U, Lancranjan I (1987) First results with ICS205–930 (5-HT3 receptor antagonist) in prevention of chemotherapy-induced emesis. Lancet i:1198

    Article  Google Scholar 

  • Leslie RA, Reynolds DJM, Newberry NR (1994) Localisation of 5-HT3 receptors. In: King FD, Jones BJ, Sanger GJ (eds) 5-Hydroxytryptamine-3 receptor antagonists. CRC, Boca Raton, pp 79–96

    Google Scholar 

  • Little JT, Broocks A, Martin A, Hill JL, Tune LE, Mack C, Cantillon M, Molchan S, Murphy DL, Sunderland T (1995) Serotonergic modulation of anticholinergic effects on cognition and behaviour in elderly humans. Psychopharmacology 120:280–288

    Article  PubMed  CAS  Google Scholar 

  • Loisy C, Beorchia S, Centonze V, Fozard JR, Schechter PJ, Tell GP (1985) Effects on migraine headache of MDL72222, an antagonist at neuronal 5-HT receptors, double-blind, placebo-controlled study. Cephalalgia 5:79–82

    Article  PubMed  CAS  Google Scholar 

  • Lummis SCR, Martin IL (1992) Solubilisation, purification and functional reconstitution of 5-hydroxytryptamine3 receptors from N1E-115 neuroblastoma cells. Mol Pharmacol 41:18–23

    PubMed  CAS  Google Scholar 

  • Lummis SCR, Kilpatrick GJ, Martin IL (1994) Molecular characterisation of 5-HT3 receptors. In: King FD, Jones BJ, Sanger GJ (eds) 5-Hydroxytryptamine-3 receptor antagonists. CRC, Boca Raton, pp 97–113

    Google Scholar 

  • Malone HM, Peters JA, Lambert JJ (1991) (+)-Tubocurarine and cocaine reveal species differences in the 5-HT3 receptors of rabbit, mouse and guinea pig nodose ganglion neurones. Br J Pharmacol 104:68P

    Google Scholar 

  • Maricq AV, Petersen AS, Brake AJ, Myers RM, Julius D (1991) Primary structure and functional expression of the 5-HT3 receptor, a serotonin-gated ion channel. Science 254:432–437

    Article  PubMed  CAS  Google Scholar 

  • Maura G, Andrioli GC, Cavazzani P, Raiteri M (1992) 5-Hydroxytryptamine3 receptor sites on cholinergic axon terminals of human cerebral cortex mediate inhibition of acetylcholine release. J Neurochem 58:2334–2337

    Article  PubMed  CAS  Google Scholar 

  • McKenzie R, Kovac A, O’Connor T, Duncalf D, Angel J, Gratz I, Tolpin E, McLeskey C, Joslyn A (1993) Comparison of ondansetron versus placebo to prevent post operative nausea and vomiting in women undergoing ambulatory gynecological surgery. Anesthiology 78:21–28

    Article  CAS  Google Scholar 

  • McKernan RM, Gillard NP, Quirk K, Kneen CO, Stevenson GI, Swain CJ, Ragan CI (1990) Purification of the 5-hydroxytryptamine 5-HT3 receptor from NCB20 cells. J Biol Chem 265:13572–13577

    PubMed  CAS  Google Scholar 

  • Meltzer HY (1991) Studies of ondansetron in schizophrenia. Satellite symposium on ondansetron, 5th world congress of biological psychiatry, Florence

    Google Scholar 

  • Minabe Y, Asby CR, Schwartz JE, Wang RY (1991) The 5-HT3 receptor antagonists LY277359 and granisetron potentiate the suppressant action of apomorphine on the basal firing rate of ventral tegmental dopamine cells. Eur J Pharmacol 209:143–150

    Article  PubMed  CAS  Google Scholar 

  • Miner WD, Sanger GJ (1986) Inhibition of cisplatin-induced vomiting by selective 5-hydroxytryptamine M-receptor antagonism. Br J Pharmacol 88:497–499

    Article  PubMed  CAS  Google Scholar 

  • Montgomery AMJ, Rose IC, Herberg LJ (1993) The effect of a 5-HT3 receptor antagonist, ondansetron, on brain stimulation reward, and its interaction with direct and indirect stimulants of central dopaminergic transmission. J Neural Trans 91:1–11

    Article  CAS  Google Scholar 

  • Murphy DL, Broocks A, Aulakh C, Pigott TA (1993) Anxiolytic effects of drugs acting on 5-HT receptor subtypes. In: Vanhoutte PM (ed) Serotonin. Kluwer Academic, Fondazione Giovanni Lrenzini, Amsterdam, pp 223–230

    Chapter  Google Scholar 

  • Naylor RJ, Rudd JA (1994) Emesis and antiemesis. In: Hanks GW, Sidebottom E (eds) Palliative medicine problem areas in pain and symptom management. Cold Spring Harbor Laboratory Press, New York, pp 117–135

    Google Scholar 

  • Neijt HC, Te Duits IJ, Vijverberg HPM (1988) Pharmacological characterisation of serotonin 5-HT3 receptor-mediated electrical response in cultured mouse neuroblastoma cells. Neuropharmacology 27:301–307

    Article  PubMed  CAS  Google Scholar 

  • Newberry NR, Cheshire SH, Gilbert MJ (1991) Evidence that the 5-HT3 receptors of the rat, mouse and guinea pig cervical ganglion may be different. Br J Pharmacol 102:615–620

    Article  PubMed  CAS  Google Scholar 

  • Newberry NR, Watkins CJ, Sprosen TS (1992) BRL 46470A antagonises 5-HT3 receptor-mediated responses on the rat vagus and on NG 108-15 cells. Br J Pharmacol 105:276P

    Google Scholar 

  • Newcomer JW, Faustman WO, Zipursky RB, Csernansky JG (1992) Zacopride in schizphrenia: a single-blind serotonin type 3 antagonist trial [letter]. Arch Gen Psychiatry 49:751–752

    Article  PubMed  CAS  Google Scholar 

  • Oakley NR, Jones BJ, Tyers MB (1988) Tolerance and withdrawal studies with diazepam and GR38032F in the rat. Br J Pharmacol 95:764P

    Google Scholar 

  • Olivier B, Mos J, Van der Heyden J, Van der Poel G, Tulp M, Slangen J, De Jong R (1992) Preclinical evidence for the anxiolytic activity of 5-HT3 receptor antagonists — a review. Stress Med 8:117–136

    Article  Google Scholar 

  • Onaivi ES, Todd S, Martin BR (1989) Behavioural effects in the mouse during and following withdrawal from ethanol ingestion and or nicotine administration. Drug Alcohol Depend 24:205–211

    Article  PubMed  CAS  Google Scholar 

  • Orwin JM, Fozard JR (1986) Blockade of the flare response to intradermal 5-hydroxytryptamine in man by MDL72222, a selective antagonist at neuronal 5-hydroxytryptamine receptors. Eur J Clin Pharmacol 30:209–212

    Article  PubMed  CAS  Google Scholar 

  • Palfreyman MG, Sorenson SM, Baron BM (1992) Antipsychotic potential of 5-HT3 antagonists. In: Meltzer HY (ed) Novel antipsychotic drugs. Raven, New York, pp 211–223

    Google Scholar 

  • Paudice P, Raiteri M (1991) Cholecystokinin release mediated by 5-HT3 receptors in rat cerebral cortex and nucleus accumbens. Br J Pharmacol 103:1790–1794

    Article  PubMed  CAS  Google Scholar 

  • Pecknold JC (1990) Platelet [3H]parocetine and [3H]imipramine binding in zacopride treated patients with generalised anxiety disorder: preliminary results, presented at the International Symposium on New Concepts in Anxiety, Castres, France, April 1990

    Google Scholar 

  • Peters J A, Hales TG, Lambert JJ (1989) Electrophysiology of 5-HT3 receptors in neuronal cell lines. Trends Pharmacol Sci 10:172–175

    Article  PubMed  CAS  Google Scholar 

  • Peters JA, Malone HM, Lambert JJ (1990) Antagonism of 5-HT3 receptor mediated currents in murine N1E-115 neuroblastoma cells by (+)-tubocurarine. Neurosci Lett 110:107–112

    Article  PubMed  CAS  Google Scholar 

  • Peters JA, Malone HM, Lambert JJ (1991) Characterisation of 5-HT3 receptor mediated electrical responses in nodose ganglion neurones and clonal neuroblastoma cells maintained in culture. In: Fozard JR, Saxena PR (eds) Serotonin: molecular biology, receptors and functional effects. Birkhauser, Basel, pp 84–94

    Chapter  Google Scholar 

  • Peters JA, Lambert JJ, Malone HM (1994) Electrophysiological studies of 5-HT3 receptors. In: King FD, Jones BJ, Sanger GJ (eds) 5-Hydroxytryptamine-3 receptor antagonists. CRC, Boca Raton, pp 115–153

    Google Scholar 

  • Pinkus LM, Gordon JC (1991) Utilisation of zacopride and its R- and S-enantiomers in studies of 5-HT3 receptor subtypes. In: Fozard JR, Saxena PR (eds) Serotonin: receptors, molecular biology and functional effects. Birkhauser, Basel, pp 439–448

    Chapter  Google Scholar 

  • Pinkus LM, Sarbin NS, Barefoot DS, Gordon JC (1989) Association of [3H]zacopride with 5-HT3 binding sites. Eur J Pharmacol 163:355–362

    Article  Google Scholar 

  • Pitsikas N, Brambilla A, Borsini F (1993) DAU 6215, a novel 5-HT3 receptor antagonist, improves performance in the aged rat in the Morris water maze task. Neurobiol Aging 14:561–564

    Article  PubMed  CAS  Google Scholar 

  • Pitsikas N, Brambilla A, Borsini F (1994) Effect of DAU 6215, a novel 5-HT3 receptor antagonist, on scopolamine induced amnesia in the rat in a spatial learning task. Pharmacol Biochem Behav 47:95–99

    Article  PubMed  CAS  Google Scholar 

  • Pratt GD, Bowery NG (1989) The 5-HT3 receptor ligand, [3H]BRL43694, binds to presynaptic sites in the nucleus tractus solitarius of the rat. Neuropharmacology 28:1367–1376

    Article  PubMed  CAS  Google Scholar 

  • Preston GC (1994) 5-HT3 antagonists and disorders of cognition. In: Rascagni G, Brunello N, Langer SZ (eds) Recent advances in the treatment of neuro-degenerative disorders and cognitive dysfunction. Karger, Basel. Int Acad Biomed Drug Res 7:89–93

    Google Scholar 

  • Preston GC, Millson DS, Ceuppens PR, Warburton DM (1991) Effects of the 5-HT3 receptor antagonist GR68755 on a scopolamine-induced cognitive deficit in healthy subjects. Br J Clin Pharmacol 32:546P

    Google Scholar 

  • Rasmussen K, Stockton ME, Czachura JR (1991) The 5-HT3 receptor antagonist zatosetron decreases the number of spontaneously active A10 dopamine neurons. Eur J Pharmacol 205:103–116

    Article  Google Scholar 

  • Richardson BP (1992) Organisation of 5-HT neurones regulating central pain. In: Bradley PB, Handley SL, Cooper SJ, Key BJ, Barnes NM, Coote JH (eds) Serotonin, CNS receptors and brain function. Pergamon, Oxford, pp 335–347

    Google Scholar 

  • Richardson BP, Engel G (1986) The pharmacology and function of 5-HT3 receptors. Trends Neurosci 9:424–428

    Article  CAS  Google Scholar 

  • Richardson BP, Engel G, Donatsch P, Stadler PA (1985) Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs. Nature 316:126–131

    Article  PubMed  CAS  Google Scholar 

  • Roberts MHT (1984) 5-Hydroxytryptamine and antinociception. Neuropharmacology 23:1529–1536

    Article  PubMed  CAS  Google Scholar 

  • Robertson B, Bevan S (1991) Properties of 5-hydroxytryptamine3 receptor-gated currents in adult rat dorsal route ganglion neurones. Br J Pharmacol 102:272–276

    Article  PubMed  CAS  Google Scholar 

  • Rodgers RJ, Shepherd JK (1992) Attenuation of defensive analgesia in male mice by 5-HT3 receptor antagonists ICS205-930, MDL72222, MDL73147F and MDL72699. Neuropharmacology 31:553–560

    Article  PubMed  CAS  Google Scholar 

  • Round AA, Wallis DI (1986) The depolarising action of 5-hydroxytryptamine on rabbit vagal afferent and sympathetic neurones and its selective blockade by ICS205-930. Br J Pharmacol 88:485–494

    Article  PubMed  CAS  Google Scholar 

  • Round A, Wallis DI (1987) Further studies on the blockade of 5-HT depolarisations of rabbit vagal afferent and sympathetic ganglion cells by MDL72222 and other antagonists. Neuropharmacology 26:39–48

    Article  PubMed  CAS  Google Scholar 

  • Rowat BMT, Merrill CF, Davies A, South V (1991) A double-blind comparison of granisetron and placebo for the treatment of acute migraine in the emergency department. Cephalgia 11:207–213

    Article  CAS  Google Scholar 

  • Rudd JA, Jordan CC, Naylor RJ (1994) Profiles of emetic action of cisplatin in the ferret: a potential model of acute and delayed emesis. Eur J Pharmacol 262:R1-R2

    Article  PubMed  CAS  Google Scholar 

  • Sanger GJ (1987) Increased gut cholinergic activity and antagonism of 5-hydroxytryptamine M-receptors by BRL24924: potential clinical importance of BRL24924. Br J Pharmacol 91:77–87

    Article  PubMed  CAS  Google Scholar 

  • Sanger GJ, Nelson DR (1989) Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL43694 (granisetron). Eur J Pharmacol 159:113–124

    Article  PubMed  CAS  Google Scholar 

  • Sanger GJ, Banner SE, Wardle KA (1994) The role of the 5-HT3 receptor in normal and disordered gastrointestinal function. In: King FD, Jones BJ, Sanger GJ (eds) 5-Hydroxytryptamine-3 receptor antagonists. CRC, Boca Raton, pp 319–358

    Google Scholar 

  • Schtrom SS, Tecot LH, Julius DJ (1993) Developmental expression of 5-HT3 receptor in RNA. Soc Neurosci Abstr 19:632

    Google Scholar 

  • Schweizer E, Rickels K (1991) Serotonergic anxiolytics: a review of their clinical efficacy. In: Rodgers RJ, Cooper SJ (eds) 5-H1A agonists, 5-HT3 antagonists and benzodiazepines: their comparative behavioural pharmacology. John Wiley and Sons, Chichester, pp 365–376

    Google Scholar 

  • Sell LA, Cowan PJ, Robson PJ (1995) Ondansetron and opiate craving: a novel pharmacological approach to addition. Br J Pharmacol 166:511–514

    CAS  Google Scholar 

  • Sellers EM, Toneatto T, Romach MK (1994) Clinical efficacy of the 5-HT3 antagonist ondansetron in alcohol abuse and dependence. Alcohol Clin Exp Res 18:879–885

    Article  PubMed  CAS  Google Scholar 

  • Sepulveda MI, Martin IL, Lummis SCR (1991) Complex actions of BRL 43694 in N1E-115 neuroblastoma cells. Symposium 5-hydroxytryptamine — CNS receptors and brain function, Birmingham, UK, abstract, p 76

    Google Scholar 

  • Smith WW, Sancilio LF, Owera-Atepo JB, Naylor RJ, Lambert LL (1988) Zacopride, a potent 5-HT3 antagonist. J Pharm Pharmacol 40:301–302

    Article  PubMed  CAS  Google Scholar 

  • Staubli U, Xu FB (1995) Effects of 5-HT3 receptor antagonism on hippocampal theta rhythm, memory, and LTP induction in the freely moving rat. J Neurosci 15:2445–2452

    PubMed  CAS  Google Scholar 

  • Sugita S, Shen KZ, North RA (1992) 5-Hydroxytryptamine is a fast excitatory transmitter at 5-HT3 receptors in rat amygdala. Neuron 8:199–203

    Article  PubMed  CAS  Google Scholar 

  • Sullivan CA, Johnson CA, Roach H, Martin RW, Stewart DK, Morrison JC (1996) A pilot study of intravenous ondansetron for hyperemesis gravidarum. Am J Obstet Gynecol 174:1565–1568

    Article  PubMed  CAS  Google Scholar 

  • Tattersall D, Newberry N, Beer MS, Rigby M, Gilbert M, Maguire JJ, Mudunktotuwa N, Duchnowski M, McKight AT, Swain CJ, Keen C, Dourish C (1992) L683,677: pharmacological profile of a novel 5-HT3 receptor antagonist. Drug Dev Res 25:17–28

    Article  CAS  Google Scholar 

  • Tecott LH, Maricq AV, Julius D (1993) Nervous system distribution of the serotonin 5-HT3 receptor in RNA. Proc Natl Acad Sci USA 90:1430–1434

    Article  PubMed  CAS  Google Scholar 

  • Tomkins DM, Costall B, Kelly ME (1990) Release of suppressed behaviour of rat on the elevated X-maze by 5-HT3 receptor antagonists injected into the basolateral amygdala. British Association for Psychopharmacology Conference, Cambridge, abstract 68

    Google Scholar 

  • Vanner S, Suprenant A (1990) Effect of 5-HT3 receptor antagonists on 5-HT and nicotinic depolarisations in guinea pig submucosal neurones. Br J Pharmacol 99:840–844

    Article  PubMed  CAS  Google Scholar 

  • Waeber C, Hoyer D, Palacios JM (1989) 5-Hydroxytryptamine3 receptors in the human brain: autoradiographic visualisation using [3H]ICS205-930. Neuroscience 31:393–400

    Article  PubMed  CAS  Google Scholar 

  • Wallis DI (1989) Interaction of 5-hydroxytryptamine with autonomic and sensory neurones. In: Fozard JR (ed) The peripheral actions of 5-hydroxytryptamine. Oxford University Press, Oxford, pp 220–246

    Google Scholar 

  • Wallis DI, Dun DJ (1988) A comparison of fast and slow depolarisations evoked by 5-HT in guinea pig coeliac ganglion cells in vitro. Br J Pharmacol 93:110–120

    Article  PubMed  CAS  Google Scholar 

  • Wallis DI, Nash H (1981) Relative activities of substances related to 5-hydroxytryptamine as depolarising agents of superior cervical ganglion cells. Eur J Pharmacol 70:381–392

    Article  PubMed  CAS  Google Scholar 

  • Wallis DI, North RA (1978) The action of 5-hydroxytryptamine on single neurones of the rabbit superior cervical ganglion. Neuropharmacology 17:1023–1028

    Article  PubMed  CAS  Google Scholar 

  • Wang RY, Ashby CR, Edwards E (1991a) Characterisation of 5-HT3-like receptors in the rat cortex: electrophysiological and biochemical studies. In: Fozard JR, Saxena PR (eds) Serotonin: molecular biology, receptors and functional effects. Birkhauser, Basel, pp 174–185

    Chapter  Google Scholar 

  • Wang RY, Ashby CR, Minabe Y (1991b) Antipsychotic potential of granisetron: electrophysiological studies. Presented at Serotonin 1991, Birmingham, UK, 14th July, abstract, p 74

    Google Scholar 

  • Wang RY, Ashby CR, Zhang JY (1992) Functional roles of 5-HT3-like receptors in the medial prefrontal cortex. In: Bradley PB, Handley SL, Cooper SJ, Key BJ, Barnes NM, Cote JH (eds) Serotonin, CNS receptors and brain function. Pergammon, New York, pp 81–96 (Advances in biosciences, vol 85)

    Google Scholar 

  • Werner P, Humbert Y, Boess F, Reid J, Jones K, Kawashima E (1993) Organisation of the 5-HT3a receptor gene and investigation of its splice variants. Soc Neurosci Abstr 19:1164

    Google Scholar 

  • White A, Corn TH, Feetham C, Faulconbridge C (1991) Ondansetron in the treatment of schizophrenia. Lancet 337:1173

    Article  PubMed  CAS  Google Scholar 

  • Wong EHF, Wu I, Eglen RM, Whiting RL (1992) Labelling of species variants of 5-HT3 receptors by a novel 5-HT3 receptor ligand. Br J Pharmacol 105:33P

    Article  Google Scholar 

  • Wozniak KM, Pert A, Linnoila M (1990) Antagonism of 5-HT3 receptors attenuates the effects of ethanol on extracellular dopamine. Eur J Pharmacol 187:287–289

    Article  PubMed  CAS  Google Scholar 

  • Yakel JL (1992) 5-HT3 receptors as cation channels. In: Hamon M (ed) Central and peripheral 5-HT3 receptors. Academic, New York, pp 163–184

    Google Scholar 

  • Yakel JL, Jackson MB (1988) 5-HT3 receptors mediate rapid responses in cultured hippocampus and a clonal cell line. Neuron 1:615–621

    Article  PubMed  CAS  Google Scholar 

  • Yakel JL, Shao XM, Jackson SM (1990) The selectivity of the channel coupled to the 5-HT3 receptor. Brain Res 533:46–52

    Article  PubMed  CAS  Google Scholar 

  • Yakel JL, Shao XM, Jackson MB (1991) Activation and desensitisation of the 5-HT3 receptor in a rat glioma × mouse neuroblastoma hybrid cell. J Physiol (Lond) 436:293–308

    PubMed  CAS  Google Scholar 

  • Yang J, Mathie A, Hille B (1992) 5-HT3 receptor channels in dissociated rat superior-cervical ganglion neurones. J Physiol (Lond) 448:237–256

    PubMed  CAS  Google Scholar 

  • Zacny JP, Apfelbaum JL, Lichtor JL, Zaragoza JG (1993) Effects of 5-hydroxytryptamine-3 antagonist ondansetron, on cigarette smoking, smoke exposure and mood in humans. Pharmacol Biochem Behav 44:387–391

    Article  PubMed  CAS  Google Scholar 

  • Zhang JY, Zeise ML, Wang RY (1994) Serotonin3 receptor agonists attenuate glutamate-induced firing in rat hippocampal CA1 pyramidal cells. Neuropharmacology 33:483–491

    Article  PubMed  CAS  Google Scholar 

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  1. B. Costall
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  1. Freie Universität Berlin, Institut für Anatomie, Königin-Luise-Str. 15, 14195, Berlin, Germany

    H. G. Baumgarten M.D.

  2. Rheinische Friedrich-Wilhelms-Universität Bonn, Institut für Pharmakologie und Toxikologie, Reuterstr. 2b, 53113, Bonn, Germany

    M. Göthert

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Costall, B., Naylor, R.J. (2000). Neuropharmacology of 5-HT3 Receptor Ligands. In: Baumgarten, H.G., Göthert, M. (eds) Serotoninergic Neurons and 5-HT Receptors in the CNS. Handbook of Experimental Pharmacology, vol 129. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-60921-3_16

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