History of Tachykinin Receptors

  • Leslie L. Iversen
Part of the The Receptors book series (REC)

Abstract

The rapid advances in molecular pharmacology in recent years have made the concept of multiple receptors and receptor subtypes for neurotransmitters and neuropeptides a commonplace. We are no longer surprised to learn that on closer examination the muscarinic receptor exists in five distinct molecular forms, encoded by separate genes (Hulme et al., 1990), or that the dopamine receptor similarly has five subtypes, some of which in turn exist in a variety of isoforms because of variable mRNA splicing (Iversen, 1992), or the existence of genetically determined minor variants (Van Tol et al., 1992). That the varied biological actions of the three mammalian tachykinins should be mediated by three different receptors is thus easily accepted—indeed, one would anticipate that such a complex family of related neuropeptides might be associated with a larger number of receptor subtypes.

Keywords

Dopamine Atropine Inositol Guanine Lactam 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Advenier, c., Naline, E., Drapeau, G., and Regoli, D. (1987) Relative potencies of neurokinins in guinea pig. Eur. J. Pharmacol 139, 133–137.PubMedCrossRefGoogle Scholar
  2. Advenier, C., Rouissi, N., Nguyen, Q. T., Emonds-Alt, X., Brelière, J-C., Neliat, G., Naline, E., and Regoli, D. (1992) Neurokinin A (NK2) receptor revisited with SR 48968, a potent nonpeptide antagonist.Biochem. Biophys. Res. Comm. 184, 1418–1424.PubMedCrossRefGoogle Scholar
  3. Appell, K. C., Fragale, B. J., Losgig, J., Singh, S., and Tomczuk, B. E. (1992) Antagonists that demonstrate species differences in neurokinin-1 receptors.Mol. Pharmacol. 11, 774–778.Google Scholar
  4. Beaujouan, J. C., Torrens, Y., Viger, A., and Glowinski, J. (1984) A new type of tachykinin binding site in the rat brain characterized by specific binding of a labeled eledoisin derivative.Mol. Pharmacol. 26, 248–254.PubMedGoogle Scholar
  5. Beaujouan, J. C., Torrens, Y., Saffroy, M., and Glowinski, J. (1986) Quantitative autoradiographic analysis of the distribution of binding sites for [125I]Bolton Hunter derivatives of eledoisin and substance P in the rat brain.Neuroscience 18, 857–875.PubMedCrossRefGoogle Scholar
  6. Burcher, E., Buck, S. H., Lovenberg, W., and 0’ Donohue T. L. (1986) Characterization and autoradiographic localization of multiple tachykinin binding sites in gastrointestinal tract and bladder.J. Pharm. Exp. Ther. 236, 819–831.Google Scholar
  7. Burcher, E., Alouan, L. A., Johnson, P. R. A., and Black, J. L. (1991) Neuropeptide gamma, the most potent contractile tachykinin in human isolated bronchus, acts via a “nonclassical” NK2receptor.Neuropeptides 20, 79–82.PubMedCrossRefGoogle Scholar
  8. Cascieri, M. A. and Liang, T. (1983) Characterization of the substance P receptor in rat brain cortex membranes and the inhibition of radioligand binding by guanine nucleotides.J. Biol. Chem. 258, 5158–5164.PubMedGoogle Scholar
  9. Cascieri, M. A., Chicchi, G. G., and Liang, T. (1985) Demonstration of two distinct tachykinin receptors in rat brain cortex.J. Biol. Chem. 260, 1501–1507.PubMedGoogle Scholar
  10. Cascieri, M. A., Chicchi, G. G., Freidinger, R. M., Dylion Colton, C., Perlow, D. S., Williams, B., Curtis, N. R., McKnight, A. T., Maguire, J. J., Veber, D. F., and Liang, T. (1986) Conformationally constrained tachykinin analogs which are selective ligands for the eledoisin binding site.Mol. Pharmacol. 29, 34–38.PubMedGoogle Scholar
  11. Couture, R. and Regoli D. (1982) Mini review: smooth muscle pharmacology of substanceP. Pharmacology 24, 1–25.Google Scholar
  12. Dion, S., D’ Orlans-Juste, P., Drapeau, G., Rhaleb, N.-E., Rouissi, N., Tousignant, C., and Regoli, D. (1987) Characterization of neurokinin receptors in various isolated organs by the use of selective agonists.Life Sciences 41, 2269–2278.PubMedCrossRefGoogle Scholar
  13. Drapeau, G., D Orlans-Juste, P., Dion, S., Rhaleb, N.-E., and Regoli, D. (1987a) Specific agonists for neurokinin B receptors.Eur. J. Pharmacol. 136, 401–403.CrossRefGoogle Scholar
  14. Drapeau, G., d’Orléans-Juste, P., Dion, S., Rhaleb, N.-E., Rouissi, N.-E., and Regoli, D. (1987b) Selective agonists for substance P and neurokinin receptors.Neuropeptides 10, 43–54.CrossRefGoogle Scholar
  15. Emonds-Alt, X., Vilain, P., Goulaouic, P., Proietto, V., Van Broeck, D., Advenier, C., Naline, E., Neliat, G., Le Fur, G., and Breliere, J. C. (1992) A potent and selective nonpeptide antagonist of the neurokinin A (NK2) receptor.Life Sciences 50, PL101–PL106.PubMedCrossRefGoogle Scholar
  16. Falconieri-Erspamer, G., Erspamer, V., and Piccinelli, D. (1980) Parallel bioassay of physalaemin and kassinin, a tachykinin dodecapeptide from the skin of the African frog kassina senegalensis.Naunyn Schmiedeberg’ s Arch. Pharmacol. 311, 61–65.CrossRefGoogle Scholar
  17. Folkers, K., Rose11, S., Chu, J.-Y., Lu, L.-A., Tang, P.-F.L., and Ljungqvist, A. (1986) Design and synthesis of antagonists of substanceP. Acta Chem. Scand. B40, 295–302.CrossRefGoogle Scholar
  18. Garret, C., Carruette, A., Fardin, V., Moussaoui, S., Peyronel, J.-F., Blanchard, J.-C., and Laduron, P.M. (1991) Pharmacological properties of a potent and selective nonpeptide substance P antagonist.Proc. Natl. Acad. Sci. USA88,10,208–10, 212.Google Scholar
  19. Gitter, B. D., Waters, D. C., Bruns, R. F., Mason, N. R., Nixon, J. A., and Jeffry Howbert, J. (1991) Species differences in affinities of nonpeptide antagonists for substance P receptors.Eur. J. Pharmacol. 197, 237–238.PubMedCrossRefGoogle Scholar
  20. Gorbulev, A., Akhundova, A., Luzuis, H., and Fahrenholz, F. (1992) Molecular cloning of substance P receptor cDNA from guinea-pig uterus.Biochim. Biophys. Acta 1131, 99–102.PubMedCrossRefGoogle Scholar
  21. Growcott, J. W., Jamieson, A., Tarpey, A. V., and Topham, L. D. (1983) Further evidence for multiple tachykinin receptors.Eur. J. Pharmacol. 86, 59–64.CrossRefGoogle Scholar
  22. Hagan, R. M., Ireland, S. J., Jordan, C. C., Beresford, I. J. M., Deal, M. J., and Ward, R. (1991) Receptor-selective, peptidase-resistant agonists at neurokinin NK-1 and NK-2 receptors: new tools for investigating neurokinin function.Neuropeptides 19, 127–135.PubMedCrossRefGoogle Scholar
  23. Hall, M. E. and Stewart, J. M. (1983) Substance P and behavior: opposite effects of N-terminal and C-terminal fragments.Peptides 4, 763–768.PubMedCrossRefGoogle Scholar
  24. Hanley, M. R., Sandberg, B.E. B., Lee, C. M., Iversen, L. L., and Wade, R. (1980) Specific binding of3H-substance P to rat brain membranes.Nature (Lond. 286, 810–812.CrossRefGoogle Scholar
  25. Hawcock, A. B., Hayes, A. G., and Tyers, M. B. (1982) Agonist effects of [D-Pro2,DPhe7,D-Trp9]substance P—evidence for different receptors.Eur. J. Pharmacol. 80, 135–138.PubMedCrossRefGoogle Scholar
  26. Holzer-Petsche, U., Schimek, E., Amann, R., and Lembeck, F. (1985In vivoandin vitroactions of mammalian tachykinins.Naunyn Schmiedeberg’s Arch. Pharmacol. 330, 130–135.CrossRefGoogle Scholar
  27. Hulme, E. C, Birdsall, N. J. M., and Buckley, N. J. (1990) Muscarinic receptor subtypes.Annu. Rev. Pharmacol. 30, 633–673.CrossRefGoogle Scholar
  28. Hunter, J. C. and Maggio, J. E. (1984) Pharmacological characterisation of a novel tachykinin isolated from mammalian spinal cord.Eur. J. Pharmacol. 97, 159–160.PubMedCrossRefGoogle Scholar
  29. Igwe, O. J., Kim, D. C., Seybold, V. S., and Larson, A. A. (1990) Specific binding of substance P aminoterminal heptapeptide [SP(1–7)] to mouse brain and spinal cord membranes.J. Neurosci. 10, 3653–3663.PubMedGoogle Scholar
  30. Iversen, L. L. (1992) Which D4 do you have?Nature (Lond. 358, 109.CrossRefGoogle Scholar
  31. Kimura, S., Katsutoshi, G., Ogawa, T., Sugita, Y., and Kanazaw, I. (1984) Pharmacological characterization of novel mammalian tachykinins, neurokinin a and neurokinin R.Neurosci. Res. 2, 97–104.PubMedCrossRefGoogle Scholar
  32. Laufer, R., Wormser, U., Friedman, Z. Y., Gilon, C., Chorev, M., and Selinger, Z. (1985) Neurokinin B is a preferred agonist for a neuronal substance P receptor and its action is antagonized by enkephalin.Proc. Natl. Acad. Sci. USA 82, 7444–7448.PubMedCrossRefGoogle Scholar
  33. Lavielle, S., Chassaing, G., Julien, S., Marquet, A., Bergstrom, L., Beaujouan, J.-C., Torrens, Y., and Glowinski, J. (1986) Specific recognition of SP orNKB receptors by analogs of SP substituted at positions 8 and 9.Eur. J. Pharmacol. 125, 461,462.PubMedCrossRefGoogle Scholar
  34. Lee, C.-M., Iversen, L. L., Hanley, M. R., and Sandberg, B. E. B. (1982) The possible existence of multiple receptors for substance P.Naunyn Schmiedeberg’s Arch. Pharmacol. 318, 281–287.CrossRefGoogle Scholar
  35. Lee, C.-M., Javitch, J. A., and Snyder, S.H. (1983) H-substance P binding to salivary gland membranes.Mol. Pharmacol. 23, 563–569.PubMedGoogle Scholar
  36. Lee, C.-M., Campbell, N. J., Williams, B. J., and Iversen, L. L. (1986) Multiple tachykinin binding sites in peripheral tissues and in brain.Eur. J. Pharmacol. 130, 209–217.PubMedCrossRefGoogle Scholar
  37. Liang, T. and Cascieri, M. A. (1981) Substance P receptor on parotid cell membranes.J. Neurosci. 1, 1133–1141.PubMedGoogle Scholar
  38. McKnight, A. T., Maguire, J. J., Varney, M. A., Williams, B. J., and Iversen, L.L. (1988a) Characterisation of tachykinin receptors using selectivity of agonists and antagonists: evidence for an NK-4 type.Regul. Pept. 22, 126.CrossRefGoogle Scholar
  39. McKnight, A. T., Maguire, J. J., Williams, B. J., Foster, A. C., Tridgett, R., and Iversen, L. L. (1988b) Pharmacological specificity of synthetic peptides a antagonists at tachykinin receptors.Regul. Pept. 22, 127.CrossRefGoogle Scholar
  40. McKnight, A. T., Maguire, J. J., Elliott, N.J., Fletcher, A. E., Foster, A. C., Tridgett, R., Williams, B. J., Longmore, J., and Iversen, L. L. (1991) Pharmacological specificity of novel, synthetic, cyclic peptides as antagonists at tachykinin receptors.Br. J. Pharmacol. 104, 355–360.PubMedCrossRefGoogle Scholar
  41. Maggi, C. A., Patacchini, R., Guiliani, S., Rovero, P., Dion, S., Regoli, D., Giachetti, A., and Meli, A. (1990) Competitive antagonists discriminate between NK2tachykinin receptor subtypes.Br. J. Pharmacol. 100, 588–592.CrossRefGoogle Scholar
  42. Maggi, C. A., Patacchini, R., Quartara, L., Rovero, P., and Santicioli, P. (1991) Tachykinin receptors in the guinea-pig isolated bronchi.Eur. J. Pharmacol. 197,167–174.PubMedCrossRefGoogle Scholar
  43. Maggi, C. A., Eglezos, A., Quartara, L., Patacchini, R., and Giachetti, A. (1992) Heterogeneity of NK-2 tachykinin receptors in hamster and rabbit smooth muscles.Regul. Pept. 37, 85–93PubMedCrossRefGoogle Scholar
  44. Masu, Y., Nakayama, K., Tamaki, H., Harada, Y., Kuno, M., and Nakanishi, S. (1987) DNA cloning of bovine substance-K receptor through oocyte expression system.Nature 329, 836–838.PubMedCrossRefGoogle Scholar
  45. Nakanishi, S. (1991) Mammalian tachykinin receptors.Annu. Rev. Neurosci. 14, 123–136.PubMedCrossRefGoogle Scholar
  46. Nawa, H., Doteuchi, M., Igano, K., Inouye, K., and Nakanishi, S. (1984) Substance K: a novel mammalian tachykinin that differs from substance P in its pharmacological profile.Life Sci. 34, 1153–1160.PubMedCrossRefGoogle Scholar
  47. Ninkovic, M., Beaujouan, J.C., Torrens, Y., Saffroy, M., Hall, M.D., and Glowinski, J. (1985) Differential localization of tachykinin receptors in rat spinal cord.Eur. J. Pharmacol. 106, 463–464.CrossRefGoogle Scholar
  48. Perrone, M. H., Diehl, R. E., and Haubrich, D. R. (1983) Binding of [3H] substance P to putative substance P receptors in rat brain membranes.Eur. J. Pharmacol. 95, 131–133.PubMedCrossRefGoogle Scholar
  49. Petitet, F., Beaujouan, J.-C., Saffroy, M., Torrens, Y., Chassaing, G., Lavielle, S., Besseyre, J., Garret, C., Curruette, A., and Glowinski, J. (1991) Further demonstration that [Pro9]-substance Pis a potent and selective ligand of NK-1 tachykinin receptors.J. Neurochem. 56, 879–889.PubMedCrossRefGoogle Scholar
  50. Petitet, F., Saffroy, M., Torrens, Y., Lavielle, S., Chassaing, G., Loeuillet, D., Glowinski, J., and Beaujouan, J.-C. (1992) Possible existence of a new tachykinin receptor subtype in the guinea pig ileum.Peptides 13, 383–388.PubMedCrossRefGoogle Scholar
  51. Piercey, M. F., Dobry, P. J. K., Einspahr, F. J., Schroeder, L. A., and Masiques, N. (1982) Use of substance P fragments to differentiate substance P receptors of different tissues.Regul. Pept. 3, 337–349.PubMedCrossRefGoogle Scholar
  52. Piercey, M. F., Dobry-Schreur, P. J. K., Masiques, N., and Schroeder, L. A. (1985) Stereospecificity of SPIandSP2substance P receptors.Life Sci. 36, 777–780.PubMedCrossRefGoogle Scholar
  53. Quirion, R. and Dam, T.-V. (1985) Multiple tachykinin receptors in guinea pig brain. High densities of substance K (neurokinin A) binding sites in the substantia nigra.Neuropeptides 6, 191–204.PubMedCrossRefGoogle Scholar
  54. Regoli, D., d’Orleans-Juste, P., Escher, E., and Mizrahi, J. (1984a) Receptors for substance P. I. The pharmacological preparations.Eur. J. Pharmacol. 97,161–170.CrossRefGoogle Scholar
  55. Regoli, D., Mizrahi, J., d’Orleans-Juste, P., and Escher, E. (1984b) Receptors for substance P. II. Classification by agonist fragments and homologues.Eur. J. Pharmacol. 97, 171–177CrossRefGoogle Scholar
  56. Regoli, D., Escher, E., Drapeau, G., d’Orleans-Juste, P., and Mizrahi, J. (1984c) Receptors for substance P. III Classification by competitive antagonists.Eur. J. Pharmacol. 97, 179–189.CrossRefGoogle Scholar
  57. Rothman, R. B., Danks, J. A., Herkenham, M., Cascieri, M. A., Chicchi, G. G., Liang, T., and Pert, C.B. (1984) Autoradiographic localization of a novel peptide binding site in rat brain using the substance P analog, eledoisin.Neuropeptides 4, 343–349.PubMedCrossRefGoogle Scholar
  58. Rovero, P., Pestellini, V., Rhaleb, N.-E., Dion, S., Rouissi, N., Tousignant, C., Télémaque, S., Drapeau, G., and Regoli, D. (1989) Structure-activity studies of Neurokinin A.Neuropeptides 13, 263–270.PubMedCrossRefGoogle Scholar
  59. Snider, R. M., Constantine, J. W., Lowe, J. A., Longo, K. P., Lebel, W. S., Woody, H. A., Drozda, S. E., Desai, M. C., Vinick, F. J., Spencer, R. W., and Hess, H.-J. (1991) A potent nonpeptide antagonist of the substance P (NK1) receptor.Science 251, 435–437.PubMedCrossRefGoogle Scholar
  60. Teichberg, V.I., Cohen, S., and Blumberg, S. (1981) Distinct classes of substance P receptors revealed by a comparison of the activities of substance P and some of its segments.Regul. Pept. 1, 327–333.PubMedCrossRefGoogle Scholar
  61. Torrens, Y., Beaujouan, J.C., Viger, A. and Glowinski, J. (1983) Properties of a125I-substance P derivative binding to synaptosomes from various brain structures and the spinal cord of the rat.Naunyn Schmiedeberg’s Arch. Pharmacol. 324, 134–139.CrossRefGoogle Scholar
  62. Torrens, Y., Lavielle, S., Chassaing, G., Marquet, A., Glowinski, J., and Beaujouan, J. C. (1984) Neuromedin K, a tool to further distinguish two central tachykinin binding sites.Eur. J. Pharmacol. 102, 381,382.Google Scholar
  63. Torrens, Y., Beaujouan, J. C., and Glowinski, J. (1985) Pharmacological characterisation of two tachykinin binding sites in the rat cerebral cortex.Neuropeptides 6, 59–70.PubMedCrossRefGoogle Scholar
  64. Van Tol, H. M. H., Wu, C. M., Guan, H.-C., Ohara, K., Bunzow, J. R., Civelli, O., Kennedy, J., Seeman, P., Niznik, H. B., and Jovanovic, V. (1992) Multiple dopamine D4 receptor variants in the human population.Nature (Lond. 358, 149–152.CrossRefGoogle Scholar
  65. Ward, P., Ewan, G. B., Jordan, C. C., Ireland, S. J., Hagan, R. M., and Brown, J. R. (1990) Potent and highly selective neurokinin antagonists.J. Med. Chem. 33, 1848–1851.PubMedCrossRefGoogle Scholar
  66. Watson, S. P. (1983) Rapid degradation of [3H]-substance Pin guinea-pig ileum and rat vas deferensin vitro. Br. J. Pharmacol. 79, 543–552.CrossRefGoogle Scholar
  67. Watson, S. P. and Iversen, L. L. (1984) H-substance P binding to guinea-pig ileum longitudinal smooth muscle membranes.Regul. Pep. 8, 273–281.CrossRefGoogle Scholar
  68. Watson, S. P., Sandberg, B. E. B., Hanley, M. R., and Iversen, L. L. (1983) Tissue selectivity of substance P alkyl esters: suggesting multiple receptors.Eur. J. Pharmacol. 87, 77–84.PubMedCrossRefGoogle Scholar
  69. Wormser, U., Laufer, R., Hart, Y., Chorev, M., Gilon, C., and Selinger, Z. (1986) Highly selective agonists for substance P receptor subtypes.EMBO J. 5, 2805–2808.PubMedGoogle Scholar

Copyright information

© Springer Science+Business Media New York 1994

Authors and Affiliations

  • Leslie L. Iversen

There are no affiliations available

Personalised recommendations