Skip to main content

Functional Neuropharmacology of Compounds Acting at 5-HT1B/D Receptors

  • Chapter

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

Abstract

The neuropharmacology of serotonin (5-HT) has been fundamentally revised in recent years with the discovery of multiple serotonin receptor subtypes. Detailed descriptions of the pharmacology of the various receptor subtypes are to be found elsewhere in this book. We review here the available data on the in vitro and in vivo neuropharmacology of the 5-HT1B/D group of receptor subtypes and attempt to identify their possible functions and potential implications in psychiatric disorders.

This is a preview of subscription content, log in via an institution.

Buying options

Chapter
USD   29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD   39.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD   54.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Learn about institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  • Auerbach SB, Rutter JJ, Juliano PJ (1991) Substituted piperazine and indole compounds increase extracellular serotonin in rat diencephalon as determined by in vivo microdialysis. Neuropharmacology 30: 307–311

    Article  PubMed  CAS  Google Scholar 

  • Bagdy G, Kalogeras KT, Szemeredi K (1992) Effect of 5-HT1C and 5-HT2 receptor stimulation on excessive grooming, penile erection and plasma oxytocin concentrations. Eur J Pharmacol 229: 9–14

    Article  PubMed  CAS  Google Scholar 

  • Bastani B, Nash F, Meltzer H (1990) Prolactin and Cortisol responses to MK-212, a serotonin agonist, in obsessive-compulsive disorder. Arch Gen Psychiatry 47: 946–951

    Article  Google Scholar 

  • Benjamin D, Lal H, Meyerson LR (1990) The effects of 5-HT1B characterizing agents in the mouse elevated plus-maze. Life Sci 47: 195–203

    Article  PubMed  CAS  Google Scholar 

  • Blier P, Bouchard C (1994) Modulation of 5-HT release in the guinea pig brain following long-term administration of antidepressant drugs. Br J Pharmacol 113: 485–495

    Article  PubMed  CAS  Google Scholar 

  • Bosker FJ, Van Esseveldt KE, Klompmakers AA, Westenberg HGM (1995) Chronic treatment with fluvoxamine by osmotic minipumps fails to induce persistent functional changes in central 5-HT1A and 5-HT1B receptors, as measured by in vivo microdialysis in dorsal hippocampus of conscious rats. Psychopharmacology 117: 358–363

    Article  PubMed  CAS  Google Scholar 

  • Brazell MP, Marsden CA, Nisbet AP, Routledge C (1985) The 5-HT1 receptor agonist RU-24969 decreases 5-hydroxytryptamine (5-HT) release and metabolism in the rat frontal cortex in vitro and in vivo. Br J Pharmacol 86: 209–216

    Article  PubMed  CAS  Google Scholar 

  • Briley M (1985) Imipramine binding: its relationship with serotonin uptake and depression. In: Green R (ed) Neuropharmacology of serotonin. Oxford University Press, Oxford, pp 50–78

    Google Scholar 

  • Briley M, Chopin P (1991) Serotonin in anxiety. Evidence from animal models. In: Sandler M, Coppen A, Harnett S (eds) 5-Hydroxytryptamine in psychiatry: a spectrum of ideas. Oxford University Press, pp 177–197

    Chapter  Google Scholar 

  • Briley M, Chopin P (1994) Is anxiety associated with a hyper- or hypo-serotonergic state? In: Palomo T, Archer T (eds) Strategies for studying brain disorders, vol 1: Depression, anxiety and drug abuse disorders. Editorial Complutence, Donoso Cortés, Madrid, pp 197–209

    Google Scholar 

  • Briley M, Moret C (1993) Neurobiological mechanisms involved in antidepressant therapies. Clin Neuropharmacol 16: 387–400

    Article  PubMed  CAS  Google Scholar 

  • Briley M, Langer SZ, Raisman R, Sechter D, Zarifìan E (1980) 3H-imipramine binding sites are decreased in platelets of untreated depressed patients. Science 209: 303–305

    Article  PubMed  CAS  Google Scholar 

  • Callaway CW, Geyer MA (1992) Tolerance and cross-tolerance to the activating effects of 3,4-methylenedioxymethamphetamine and a 5-hydroxytryptamine1B agonist. J Pharmacol Exp Ther 263: 318–326

    PubMed  CAS  Google Scholar 

  • Callaway CW, Rempel N, Peng RY, Geyer MA (1992) Serotonin 5-HT(1)- like receptors mediate hyperactivity in rats induced by 3,4- methylenedioxymethamphetamine. Neuropsychopharmacology 7: 113–127

    PubMed  CAS  Google Scholar 

  • Carlsson A, Davis JN, Kehr W, Lindqvist M, Atack CV (1972) Simultaneous measurement of tyrosine and tryptophan hydroxylase activities in brain in vivo using an inhibitor of the aromatic amino acid decarboxylase. Naunyn Schmiedebergs Arch Pharmacol 275: 153–168

    Article  PubMed  CAS  Google Scholar 

  • Charney DS, Goodman WK, Price LH, Woods SW, Rasmussen SA, Heninger GR (1988) Serotonin function in obsessive-compulsive disorder. Arch Gen Psychiatry 45: 177–185

    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 

  • Chopin P, Moret C, Briley M (1994) Neuropharmacology of 5-hydroxytryptamine1B/D receptor ligands. Pharmacol Ther 62: 385–405

    Article  PubMed  CAS  Google Scholar 

  • Deacon R, Gardner CR (1986) Benzodiazepine and 5-HT ligands in a rat conflict test. Br J Pharmacol 88: 330P

    Google Scholar 

  • De Souza RJ, Goodwin GM, Green AR, Heal DJ (1986) Effect of chronic treatment with 5-HT1 agonist (8-OH-DPAT and RU 24969) and antagonist (ipsapirone) drugs on the behavioural responses of mice to 5-HT1 and 5-HT2 agonists. Br J Pharmacol 89: 377–384

    Article  PubMed  Google Scholar 

  • Di Chiara G (1990) In vivo brain dialysis of neurotransmitters. Trends Pharmacol Sci 11: 116–121

    Article  PubMed  Google Scholar 

  • Dolberg OT, Sasson Y, Cohen R, Zohar J (1995) The relevance of behavioral probes in obsessive-compulsive disorder. Eur Neuropsychopharmacol 5: 161–162

    Article  Google Scholar 

  • Edwards E, Harkins K, Wright G, Henn FA (1991) 5-HT1B receptors in an animal model of depression. Neuropharmacology 30: 101–105

    Article  PubMed  CAS  Google Scholar 

  • Engel G, Göthert M, Hoyer D, Schlicker E, Hillenbrand K (1986) Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sites. Naunyn Schmiedebergs Arch Pharmacol 332: 1–7

    Article  PubMed  CAS  Google Scholar 

  • Feighner JP, Boyer WF (1991) Selective serotonin reuptake inhibitors. Wiley, Chichester

    Google Scholar 

  • Fernandez-Guasti A, Escalante A (1991) Role of presynaptic serotonergic receptors on the mechanism of action of 5-HT1A and 5-HT1B agonists on masculine sexual behaviour: physiological and pharmacological implications. J Neural Trans 85: 95–107

    Article  CAS  Google Scholar 

  • Fernandez-Guasti A, Rodriguez-Manzo G (1992) Further evidence showing that the inhibitory action of serotonin on rat masculine sexual behavior is mediated after the stimulation of 5-HT1B receptor. Pharmacol Biochem Behav 42: 529–533

    Article  PubMed  CAS  Google Scholar 

  • Finberg JP, Vardi Y (1990) Inhibitory effect of 5-hydroxytryptamine on penile erectile function in the rat. Br J Pharmacol 101: 698–702

    Article  PubMed  CAS  Google Scholar 

  • Franceschini R, Cataldi A, Garibaldi A, Cianciosi P, Scordamaglia A, Barreca T, Rolandi E (1994) The effects of sumatriptan on pituitary secretion in man. Neuropharmacology 33: 235–239

    Article  PubMed  CAS  Google Scholar 

  • Francès H (1988) New animal model of social behavioural deficit: reversal by drugs. Pharmacol Biochem Behav 29: 467–470

    Article  PubMed  Google Scholar 

  • Francès H, Khidichian F (1990) Chronic but not acute antidepressants interfere with serotonin (5-HT1B) receptors. Eur J Pharmacol 179: 173–176

    Article  PubMed  Google Scholar 

  • Francès H, Monier C (1991a) Isolation increases a behavioral response to the selective 5-HT1B agonist CGS 12066B. Pharmacol Biochem Behav 40: 279–281

    Article  PubMed  Google Scholar 

  • Francès H, Monier C (1991b) Tolerance to the effect of serotonergic (5-HT1B) agonists in the isolation-induced social behavioral deficit test. Neuropharmacology 30: 623–627

    Article  PubMed  Google Scholar 

  • Frances H, Khidichian F, Monier C (1990a) Benzodiazepines impair a behavioral effect induced by stimulation of 5-HT1B receptors. Pharmacol Biochem Behav 35: 841–845

    Article  PubMed  CAS  Google Scholar 

  • Francès H, Khidichian F, Monier C (1990b) Increase in the isolation-induced social behavioral deficit by agonists at 5-HT1A receptors. Neuropharmacology 29: 103–107

    Article  PubMed  Google Scholar 

  • Galzin AM, Poirier MF, Lista A, Chodkiewicz JP, Blier P, Ramdine R, Loo H, Roux FX, Redondo A, Langer SZ (1992) Characterization of the 5-hydroxytryptamine receptor modulating the release of 5-[3H]hydroxytryptamine in slices of the human neocortex. J Neurochem 59: 1293–1301

    Article  PubMed  CAS  Google Scholar 

  • Garattini S, Mennini T, Samanin R (1989) Reduction of food intake by manipulation of central serotonin. Current experimental results. Br J Psychiatry 8: 41–51

    Google Scholar 

  • Gibbons JL, Barr GA, Bridger WH, Leibowitz SF (1979) Manipulations of dietary tryptophan: effects on mouse killing and brain serotonin in the rat. Brain Res 169: 139–153

    Article  PubMed  CAS  Google Scholar 

  • Giral P, Martin P, Soubrié P, Simon P (1988) Reversal of helpless behavior in rats by putative 5-HT1A agonists. Biol Psychiatry 23: 237–242

    Article  PubMed  CAS  Google Scholar 

  • Gorzalka BB, Mendelson SD, Watson NV (1990) Serotonin receptor subtypes and sexual behavior. In: Whitaker-Azmitia PM, Peroutka SJ (eds) The neuropharmacology of serotonin. New York Academy of Sciences, New York, pp 435–446

    Google Scholar 

  • Green AR, Guy AP, Gardner CR (1984) The behavioural effects of RU 24969, a suggested 5-HT1 receptor agonist in rodents and the effect on the behaviour of treatments with antidepressants. Neuropharmacology 23: 655–661

    Article  PubMed  CAS  Google Scholar 

  • Grignaschi G, Samanin R (1992) Role of 5-HT receptors in the effect of d-fenfluramine on feeding patterns in the rat. Eur J Pharmacol 212: 287–289

    Article  PubMed  CAS  Google Scholar 

  • Hartig PR, Branchek TA, Weinshank RL (1992) A subfamily of 5-HT1D receptor genes. Trends Pharmacol Sci 13: 152–159

    Article  PubMed  CAS  Google Scholar 

  • Hartig PR, Hoyer D, Humphrey PPA, Martin GR (1996) Alignment of receptor nomenclature with the human genome: classification of 5-HT1B and 5-HT1D receptor subtypes. Trends Pharmacol Sci 17: 103–105

    Article  PubMed  CAS  Google Scholar 

  • Herdman JRE, Delva NJ, Hockney RE, Campling GM, Cowen PJ (1994) Neuroendocrine effects of sumatriptan. Psychopharmacology 113: 561–564

    Article  PubMed  CAS  Google Scholar 

  • Hjorth S, Tao R (1991) The putative 5-HT1B receptor agonist CP 93129 suppresses rat hippocampal 5-HT release in vivo — comparison with RU 24969. Eur J Pharmacol 209: 249–252

    Article  PubMed  CAS  Google Scholar 

  • Hjorth S, Suchowski CS, Galloway MP (1995) Evidence for 5-HT autoreceptor- mediated, nerve impulse-independent, control of 5-HT synthesis in the rat brain. Synapse 19: 170–176

    Article  PubMed  CAS  Google Scholar 

  • Hollander E, DeCaria CM, Nitescu A (1992) Serotonergic function in obsessive- compulsive disorder. Arch Gen Psychiatry 49: 21–28

    Article  PubMed  CAS  Google Scholar 

  • Hoyer D, Middlemiss DN (1989) Species differences in the pharmacology of terminal 5-HT autoreceptors in mammalian brain. Trends Pharmacol Sci 10: 130–132

    Article  PubMed  CAS  Google Scholar 

  • Hoyer D, Schoeffter P, Waeber C, Palacios JM (1990) Serotonin 5-HT1D receptors. Ann N Y Acad Sci 600: 168–182

    Article  PubMed  CAS  Google Scholar 

  • Hutson PH, Bristow LJ, Cunningham JR, Hogg JE, Longmore J, Murray F, Pearce D, Razzaque Z, Saywell K, Tricklebank MD, Young L (1995) The effects of GR127935, a putative 5-HT1D receptor antagonist, on brain 5-HT metabolism, extracellular 5-HT concentration and behaviour in the guinea pig. Neuropharmacology 34: 383–392

    Article  PubMed  CAS  Google Scholar 

  • Imperato A, Di Chiara G (1985) Dopamine release and metabolism in awake rats after systemic neuroleptics as studied by trans-striatal dialysis. J Neurosci 5: 297–306

    PubMed  CAS  Google Scholar 

  • Imperato A, Tanda G, Frau R, Di Chiara G (1988) Pharmacological profile of dopamine receptor agonists as studied by brain dialysis in behaving rats. J Pharmacol Exp Ther 245: 257–264

    PubMed  CAS  Google Scholar 

  • Kennett GA, Curzon G (1988a) Evidence that hypophagia induced by mCPP and TFMPP requires 5-HT1C and 5-HT1B receptors; hypophagia induced by RU 24969 only requires 5-HT1B receptors. Psychopharmacology 96: 93–100

    Article  PubMed  CAS  Google Scholar 

  • Kennett GA, Curzon G (1988b) Evidence that mCPP may have behavioural effects mediated by central 5-HT1C receptors. Br J Pharmacol 94: 137–144

    Article  PubMed  CAS  Google Scholar 

  • Kennett GA, Dourish CT, Curzon G (1987) 5-HT1B agonists induce anorexia at a post synaptic site. Eur J Pharmacol 141: 429–435

    Article  PubMed  CAS  Google Scholar 

  • Koe BK, Lebel LA, Burkhart CA, Macor JE (1990) CP-93,129, a new serotonergic ligand with marked affinity and high selectivity for 5-HT1B receptors. Soc Neurosci Abstr 16: 1035

    Google Scholar 

  • Koe BK, Nielsen JA, Macor JE, Heym J (1992) Biochemical and behavioral studies of the 5-HT1B receptor agonist, CP-94,253. Drug Dev Res 26: 241–250

    Article  CAS  Google Scholar 

  • Langer SZ, Moret C (1982) Citalopram antagonizes the stimulation by lysergic acid diethylamide of presynaptic inhibitory serotonin autoreceptors in the rat hypothalamus. J Pharmacol Exp Ther 222: 220–226

    PubMed  CAS  Google Scholar 

  • Lawrence AJ, Marsden CA (1992) Terminal autoreceptor control of 5- hydroxytryptamine release as measured by in vivo microdialysis in the conscious guinea pig. J Neurochem 58: 142–146

    Article  PubMed  CAS  Google Scholar 

  • Limberger N, Deicher R, Starke K (1991) Species differences in presynaptic serotonin autoreceptors: mainly 5-HT1B but possibly in addition 5-HT1D in the rat, 5-HT1D in the rabbit and guinea pig cortex. Naunyn Schmiedebergs Arch Pharmacol 343: 353–364

    Article  PubMed  CAS  Google Scholar 

  • Lucki I, Frazer A (1982) Behavioural effects of indole and piperazine-type serotonin receptor agonists. Soc Neurosci Abstr 8: 101

    Google Scholar 

  • Macor JE, Burkhart CA, Heym JH, Ives JL, Lebel LA, Newman ME, Nielsen JA, Rya B (1990) 3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo<3,2-b>pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole. J Med Chem 33: 2087–2093

    Article  PubMed  CAS  Google Scholar 

  • Malick JB, Barnett A (1976) The role of serotonergic pathways in isolation-induced aggression in mice. Pharmacol Biochem Behav 5: 55–61

    Article  PubMed  CAS  Google Scholar 

  • Marsden CA, Martin KF, Brazell MP, Maidment NT (1987) In vivo voltammetry. Application to the identification of dopamine and 5-hydroxytryptamine receptors. In: Justice JB (ed) Voltammetry in the Neurosciences. Humana, Clifton, pp 209–237

    Chapter  Google Scholar 

  • Martin KF, Marsden CA (1987) In vivo voltammetry in the suprachiasmatic nucleus of the rat: effects of RU 24969, methiothepin and ketanserin. Eur J Pharmacol 121: 135–139

    Article  Google Scholar 

  • Martin KF, Hannon S, Phillips I, Heal DJ (1992) Opposing roles for 5-HT1B and 5-HT3 receptors in the control of 5-HT release in rat hippocampus in vivo. Br J Pharmacol 106: 139–142

    Article  PubMed  CAS  Google Scholar 

  • Martin P, Puech AJ (1991) Is there a relationship between 5-HT1B receptors and the mechanisms of action of antidepressant drugs in the learned helplessness paradigm in rats? Eur J Pharmacol 192: 193–196

    Article  PubMed  CAS  Google Scholar 

  • Martin P, Beninger RJ, Hamon M, Puech A J (1990) Antidepressant-like action of 8- OH-DPAT, a 5-HT1A agonist, in the learned helplessness paradigm: evidence for a postsynaptic mechanism. Behav Brain Res 38: 135–144

    Article  PubMed  CAS  Google Scholar 

  • Maura G, Thellung S, Andrioli GC, Ruelle A, Raiteri M (1993) Release-regulating serotonin 5-HT1D autoreceptors in human cerebral cortex. J Neurochem 60: 1179–1182

    Article  PubMed  CAS  Google Scholar 

  • McMillen BA, Da Vanzo EA, Scott SM, Song AH (1988) N-Alkyl-substituted aryl- piperazine drugs: relationship between affinity for serotonin receptors and inhibition of aggression. Drug Dev Res 12: 53–62

    Article  CAS  Google Scholar 

  • McNamara MG, Kelly JP, Leonard BE (1995) Some behavioural effects of methiothepin in the olfactory bulbectomised rat model of depression. Med Sci Res 23: 583–585

    CAS  Google Scholar 

  • Meert TF, Colpaert FC (1986) The shock probe conflict procedure. A new assay responsive to benzodiazepines, barbiturates and related compounds. Psychopharmacology 88: 445–450

    Article  PubMed  CAS  Google Scholar 

  • Middlemiss DN (1986) Blockade of the central 5-HT autoreceptor by β-adrenoceptor antagonists. Eur J Pharmacol 120: 51–54

    Article  PubMed  CAS  Google Scholar 

  • Middlemiss DN (1988) Autoreceptors regulating serotonin release. In: Sanders-Bush E (ed) The serotonin receptors. Humana, Clifton, pp 210–224

    Google Scholar 

  • Mittman SM, Geyer MA (1989) Effects of 5-HT1A agonists on locomotor and investigatory behaviors in rats differ from those of hallucinogens. Psychopharmacology 98: 321–329

    Article  PubMed  CAS  Google Scholar 

  • Monsma FJ, Yong Shen JR, Ward RP, Hamblin MW, Sibley DR (1993) Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol 43: 320–327

    PubMed  CAS  Google Scholar 

  • Moret C (1985) Pharmacology of the serotonin autoreceptor. In: Green AR (ed) Neuropharmacology of serotonin. Oxford University Press, Oxford, pp 21–49

    Google Scholar 

  • Moret C, Briley M (1986) Dihydroergocristine-induced stimulation of the 5-HT autoreceptor in the hypothalamus of the rat. Neuropharmacology 25: 169–174

    Article  PubMed  CAS  Google Scholar 

  • Moret C, Briley M (1990) Serotonin autoreceptor subsensitivity and antidepressant activity. Eur J Pharmacol 180: 351–356

    Article  PubMed  CAS  Google Scholar 

  • Moret C, Briley M (1993) Which 5-HT receptors are involved in the modulation of 5- HT synthesis by the 5-HT uptake blocker, citalopram? Br J Pharmacol 108: 95P

    Google Scholar 

  • Moret C, Briley M (1996) Effects of acute and repeated administration of citalopram on extracellular levels of serotonin in rat brain. Eur J Pharmacol 295: 189–197

    Article  PubMed  CAS  Google Scholar 

  • Mos J, Olivier B, Poth M, Van Aken H (1992) The effects of intraventricular administration of eltoprazine, 1-(3-trifluoromethylphenyl)piperazine hydrochloride, and 8-hydroxy-2-(di-n-propylamino)tetralin on resident intruder aggression in the rat. Eur J Pharmacol 212: 295–298

    Article  PubMed  CAS  Google Scholar 

  • Mota A, Bento A, Peñalva A, Pombo M, Dieguez C (1995) Role of the serotonin receptor subtype 5-HT1D on basal and stimulated growth hormone secretion. J Clin Endocrinol Metab 80: 1973–1977

    Article  PubMed  CAS  Google Scholar 

  • Oberlander C, Demassey Y, Verdu A, van de Velde D, Bardelay C (1987) Tolerance to the serotonin 5 HT1 agonist RU 24969 and effects on dopaminergic behaviour. Eur J Pharmacol 139: 205–214

    Article  PubMed  CAS  Google Scholar 

  • O’Connor JJ, Kruk ZL (1994) Effects of 21 days treatment with fluoxetine on stimulated endogenous 5-hydroxytryptamine overflow in the rat dorsal raphe and suprachiasmatic nucleus studied using fast cyclic voltammetry in vitro. Brain Res 640: 328–335

    Article  PubMed  Google Scholar 

  • Offord SJ, Ordway GA, Frazer A (1988) Application of [125I]iodocyanopindolol to measure 5-hydroxytryptamine (1B) receptors in the brain of the rat. J Pharmacol Exp Ther 244: 144–153

    PubMed  CAS  Google Scholar 

  • Ögren S-O, Holm A-C, Renyi AL, Ross SB (1980) Anti-aggressive effect of zimelidine in isolated mice. Acta Pharmacol Toxicol 47: 71–74

    Article  Google Scholar 

  • Olivier B, Mos J (1992) Rodent models of aggressive behavior and serotonergic drugs. Prog Neuropsychopharmacol Biol Psychiatry 16: 847–870

    Article  PubMed  CAS  Google Scholar 

  • Olivier B, Mos J, van der Heyden JAM, Hartog J (1989) Serotonergic modulation of social interactions in isolated male mice. Psychopharmacology 97: 154–156

    Article  PubMed  CAS  Google Scholar 

  • Pellow S, Johnston AL, File SE (1987) Selective agonists and antagonists for 5- hydroxytryptamine receptor subtypes, and interactions with yohimbine and FG 7142 using the elevated plus-maze test in the rat. J Pharm Pharmacol 39: 917–928

    Article  PubMed  CAS  Google Scholar 

  • Petty F, Kramer G, Wilson L (1992) Prevention of learned helplessness — in vivo correlation with cortical serotonin. Pharmacol Biochem Behav 43: 361–367

    Article  PubMed  CAS  Google Scholar 

  • Pigott TA, Zohar J, Hill JL (1991) Metergoline blocks the behavioral and neuroendocrine effects of orally administered m-chlorophenylpiperazine in patients with obsessive-compulsive disorder. Biol Psychiatry 29: 418–426

    Article  PubMed  CAS  Google Scholar 

  • Pigott TA, Murphy DL, Brooks A (1993) Pharmacological probes in OCD: support for selective 5-HT dysregulation. Presented at the 1st international obsessive compulsive disorder congress, Capri, Italy, 12–13 March

    Google Scholar 

  • Piñeyro G, Castanon N, Hen R, Blier P (1995) Regulation of 5-HT release in 5-HT1B knock-out mice: experiments in hippocampal, frontal cortex and midbrain raphe slices. Soc Neurosci Abstr 21: 1368

    Google Scholar 

  • Rempel N, Callaway CW, Geyer MA (1993) Serotonin-1B receptor activation mimics behavioural effects of presynaptic serotonin release. Neuropsychopharmacology 8:201–211

    PubMed  CAS  Google Scholar 

  • Roberts C, Thorn L, Price GW, Middlemiss DN, Jones BJ (1994) Effect of the selective 5-HT1D receptor antagonist, GR 127935, on in vivo 5-HT release, synthesis and turnover in the guinea pig frontal cortex. Br J Pharmacol 112: 488P

    Google Scholar 

  • Rodgers RJ, Cole JC, Cobain MR, Daly P, Doran PJ, Eells JR, Wallis P (1992) Anxiogenic-like effects of fluprazine and eltoprazine in the mouse elevated plusmaze: profile comparisons with 8-OH-DPAT. CGS 12066B, TFMPP and mCPP. Behav Pharmacol 3: 621–634

    PubMed  CAS  Google Scholar 

  • Sánchez C, Arnt J, Hyttel J, Moltzen EK (1993) The role of serotonergic mechanisms in inhibition of isolation-induced aggression in male mice. Psychopharmacology 110: 53–59

    Article  PubMed  Google Scholar 

  • Schlicker E, Fink K, Göthert M, Hoyer D, Molderings G, Roschke I, Schoeffter P (1989) The pharmacological properties of the presynaptic serotonin autoreceptor in the pig brain cortex conform to the 5-HT1D receptor subtype. Naunyn Schmiedebergs Arch Pharmacol 340: 45–51

    PubMed  CAS  Google Scholar 

  • Schlicker E, Werner U, Hamon M, Gozlan H, Nickel B, Szelenyi I, Göthert M (1992) Anpirtoline, a novel, highly potent 5-HT1B receptor agonist with antinociceptive/ antidepressant-like actions in rodents. Br J Pharmacol 105: 732–738

    Article  PubMed  CAS  Google Scholar 

  • Schoups AA, De Potter WP (1988) Species dependence of adaptations at the pre- and postsynaptic serotonergic receptors following long-term antidepressant drug treatment. Biochem Pharmacol 37: 4451–4460

    Article  PubMed  CAS  Google Scholar 

  • Sharp T, Ljungberg T, Zetterström T, Ungerstedt U (1986) Intracerebral dialysis coupled to a novel activity box — a method to monitor dopamine release during behaviour. Pharmacol Biochem Behav 24: 1755–1759

    Article  PubMed  CAS  Google Scholar 

  • Sharp T, Bramwell SR, Hjorth S, Grahame-Smith DG (1989a) Pharmacological characterization of 8-OH-DPAT-induced inhibition of rat hippocampal 5-HT release in vivo as measured by microdialysis. Br J Pharmacol 98: 989–997

    Article  PubMed  CAS  Google Scholar 

  • Sharp T, Bramwell ST, Grahame-Smith DG (1989b) 5-HT1 agonists reduce 5- hydroxytryptamine release in rat hippocampus in vivo as determined by brain microdialysis. Br J Pharmacol 96: 283–290

    Article  PubMed  CAS  Google Scholar 

  • Sherman AD, Petty F (1984) Learned helplessness decreases 3H-imipramine binding in rat cortex. J Affect Disord 6: 25–32

    Article  PubMed  CAS  Google Scholar 

  • Sherman AD, Allers GL, Petty F, Henn FA (1979) A neuropharmacologically relevant animal model of depression. Neuropharmacology 18: 891–894

    Article  PubMed  CAS  Google Scholar 

  • Sijbesma H, Schipper J, De Kloet ER, Mos J, Van Aken H, Olivier B (1991) Postsynaptic 5-HT1 receptors and offensive aggression in rats: a combined behavioural and autoradiographic study with eltoprazine. Pharmacol Biochem Behav 38: 447–458

    Article  PubMed  CAS  Google Scholar 

  • Sleight AJ, Smith RJ, Marsden CA, Palfreyman MG (1989) The effects of chronic treatment with amitriptyline and MDL 72394 on the control of 5-HT release in vivo. Neuropharmacology 28: 477–480

    Article  PubMed  CAS  Google Scholar 

  • Sleight AJ, Cervenka A, Peroutka SJ (1990) In vivo effects of sumatriptan (GR-43175) on extracellular levels of 5-HT in the guinea pig. Neuropharmacology 29: 511–513

    Article  PubMed  CAS  Google Scholar 

  • Sleight AJ, Carolo C, Petit N, Zwingelstein C, Bourson A (1995) Identification of 5- hydroxytryptamine7 receptor binding sites in rat hypothalamus: sensitivity to chronic antidepressant treatment. Mol Pharmacol 47: 99–103

    PubMed  CAS  Google Scholar 

  • Stanley M, Vigilio J, Gershon S (1982) Tritiated imipramine binding sites are decreased in the frontal cortex of suicides. Science 216: 1337–1339

    Article  PubMed  CAS  Google Scholar 

  • Starke K, Göthert M, Kilbinger H (1989) Modulation of neurotransmitter release by presynaptic autoreceptors. Physiol Rev 69: 864–989

    PubMed  CAS  Google Scholar 

  • Starkey SJ, Skingle M (1994) 5-HT1D as well as 5-HT1A autoreceptors modulate 5-HT release in the guinea pig dorsal raphé nucleus. Neuropharmacology 33: 393–402

    Article  PubMed  CAS  Google Scholar 

  • Tricklebank MD, Middlemiss DN, Neill J (1986) Pharmacological analysis of the behavioural and thermoregulatory effects of the putative 5-HT1 receptor agonist, RU 24969, in the rat. Neuropharmacology 25: 877–886

    Article  PubMed  CAS  Google Scholar 

  • Tsou A, Kosaka A, Bach C, Zuppan P, Yee C, Tom L, Alvarez R, Ramsey S, Bonhaus DW, Stefanich E, Jakeman L, Eglen RM, Chan HW (1994) Cloning and expression of a 5-hydroxytryptamine7 receptor positively coupled to adenylyl cyclase. J Neurochem 63: 456–464

    Article  PubMed  CAS  Google Scholar 

  • Ungerstedt U (1984) Measurement of neurotransmitter release by intracranial dialysis. In: Marsden CA (ed) Measurement of neurotansmitter release in vivo. Wiley, New York, pp 81–105

    Google Scholar 

  • Vandijken HH, Mos J, van der Heyden JAM, Tilders FJH (1992a) Characterization of stress-induced long-term behavioural changes in rats — evidence in favor of anxiety. Physiol Behav 52: 945–951

    Article  CAS  Google Scholar 

  • Vandijken HH, van der Heyden JAM, Mos J, Tilders FJH (1992b) Inescapable footshocks induce progressive and long-lasting behavioural changes in male rats. Physiol Behav 51: 787–794

    Article  CAS  Google Scholar 

  • Vergé D, Daval G, Marcinkiewicz M, Patey A, El Mestikawy S, Gozlan S, Hamon M (1986) Quantitative autoradiography of multiple 5-HT1 receptor subtypes in the brain of control or 5,7-dihydroxytryptamine-treated rats. J Neurosci 6: 3474–3482

    PubMed  Google Scholar 

  • Waeber C, Dietl MM, Hoyer D, Palacios JM (1989) 5-HT1 receptors in the vertebrate brain: regional distribution examined by autoradiography. Naunyn Schmiedebergs Arch Pharmacol 340: 486–494

    PubMed  CAS  Google Scholar 

  • Wieland S, Lucki I (1990) Antidepressant-like activity of 5-HT1A agonists measured with the forced swim test. Psychopharmacology 101: 497–504

    Article  PubMed  CAS  Google Scholar 

  • Wilkinson LO, Middlemiss DN (1992) Metitepine distinguishes two receptors mediating inhibition of [3H]-5-hydroxytryptamine release in guinea pig hippocampus. Naunyn Schmiedebergs Arch Pharmacol 345: 696–699

    Article  PubMed  CAS  Google Scholar 

  • Wing LL, Tapson GS, Geyer MA (1990) 5-HT2 mediation of acute behavioral effects of hallucinogens in rats. Psychopharmacology 100: 417–425

    Article  PubMed  CAS  Google Scholar 

  • Zohar J, Mueller EA, Insel TR (1987) Serotonin responsivity in obsessive compulsive disorder. Arch Gen Psychiatry 44: 946–951

    Article  PubMed  CAS  Google Scholar 

  • Zohar J, Insel TR, Zohar-Kadoush RC, Hill JL, Murphy DL (1988) Serotonergic responsivity in obsessive-compulsive disorder: effects of clomipramine treatment. Arch Gen Psychiatry 45: 167–172

    Article  PubMed  CAS  Google Scholar 

Download references

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 2000 Springer-Verlag Berlin Heidelberg

About this chapter

Cite this chapter

Briley, M., Chopin, P., Marien, M., Moret, C. (2000). Functional Neuropharmacology of Compounds Acting at 5-HT1B/D Receptors. 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_10

Download citation

  • DOI: https://doi.org/10.1007/978-3-642-60921-3_10

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-540-66715-5

  • Online ISBN: 978-3-642-60921-3

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics