Skip to main content
NCBI home page
Journal of Psychiatry & Neuroscience: JPN logoLink to Journal of Psychiatry & Neuroscience: JPN
. 1995 May;20(3):215–225.

Phosphoinositide system-linked serotonin receptor subtypes and their pharmacological properties and clinical correlates.

S C Pandey 1, J M Davis 1, G N Pandey 1
PMCID: PMC1188687  PMID: 7786883

Abstract

Serotonergic neurotransmission represents a complex mechanism involving pre- and post-synaptic events and distinct 5-HT receptor subtypes. Serotonin (5-HT) receptors have been classified into several categories, and they are termed as 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6 and 5-HT7 type receptors. 5-HT1 receptors have been further subdivided into 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E and 5-HT1F. 5-HT2 receptors have been divided into 5-HT2A, 5-HT2B and 5-HT2C receptors. All 5-HT2 receptor subtypes are linked to the multifunctional phosphoinositide (PI) signalling system. 5-HT3 receptors are considered ion-gated receptors and are also linked to the PI signalling system by an unknown mechanism. The 5-HT2A receptor subtype is the most widely studied of the 5-HT receptors in psychiatric disorders (for example, suicide, depression and schizophrenia) as well as in relation to the mechanism of action of antidepressant drugs. The roles of 5-HT2C and 5-HT3 receptors in psychiatric disorders are less clear. These 5-HT receptors also play an important role in alcoholism. It has been shown that 5-HT2A, 5-HT2C and 5-HT3 antagonists cause attenuation of alcohol intake in animals and humans. However, the exact mechanisms are unknown. The recent cloning of the cDNAs for 5-HT2A, 5-HT2C and 5-HT3 receptors provides the opportunity to explore the molecular mechanisms responsible for the alterations in these receptors during illness as well as pharmacotherapy. This review article will focus on the current research into the pharmacological properties, molecular biology, and clinical correlates of 5-HT2A, 5-HT2C and 5-HT3 receptors.

Full text

PDF
215

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Andree T. H., Mikuni M., Tong C. Y., Koenig J. I., Meltzer H. Y. Differential effect of subchronic treatment with various neuroleptic agents on serotonin2 receptors in rat cerebral cortex. J Neurochem. 1986 Jan;46(1):191–197. doi: 10.1111/j.1471-4159.1986.tb12944.x. [DOI] [PubMed] [Google Scholar]
  2. Arora R. C., Meltzer H. Y. Increased serotonin2 (5-HT2) receptor binding as measured by 3H-lysergic acid diethylamide (3H-LSD) in the blood platelets of depressed patients. Life Sci. 1989;44(11):725–734. doi: 10.1016/0024-3205(89)90384-6. [DOI] [PubMed] [Google Scholar]
  3. Arora R. C., Meltzer H. Y. Serotonergic measures in the brains of suicide victims: 5-HT2 binding sites in the frontal cortex of suicide victims and control subjects. Am J Psychiatry. 1989 Jun;146(6):730–736. doi: 10.1176/ajp.146.6.730. [DOI] [PubMed] [Google Scholar]
  4. Barnes N. M., Costall B., Naylor R. J. [3H]zacopride: ligand for the identification of 5-HT3 recognition sites. J Pharm Pharmacol. 1988 Aug;40(8):548–551. doi: 10.1111/j.2042-7158.1988.tb05300.x. [DOI] [PubMed] [Google Scholar]
  5. Berridge M. J. Inositol trisphosphate and diacylglycerol: two interacting second messengers. Annu Rev Biochem. 1987;56:159–193. doi: 10.1146/annurev.bi.56.070187.001111. [DOI] [PubMed] [Google Scholar]
  6. Biegon A., Grinspoon A., Blumenfeld B., Bleich A., Apter A., Mester R. Increased serotonin 5-HT2 receptor binding on blood platelets of suicidal men. Psychopharmacology (Berl) 1990;100(2):165–167. doi: 10.1007/BF02244400. [DOI] [PubMed] [Google Scholar]
  7. Bleich A., Brown S. L., Kahn R., van Praag H. M. The role of serotonin in schizophrenia. Schizophr Bull. 1988;14(2):297–315. doi: 10.1093/schbul/14.2.297. [DOI] [PubMed] [Google Scholar]
  8. Briley M. S., Langer S. Z., Raisman R., Sechter D., Zarifian E. Tritiated imipramine binding sites are decreased in platelets of untreated depressed patients. Science. 1980 Jul 11;209(4453):303–305. doi: 10.1126/science.7384806. [DOI] [PubMed] [Google Scholar]
  9. Buckholtz N. S., Zhou D. F., Tabakoff B. Ethanol does not affect serotonin receptor binding in rodent brain. Alcohol. 1989 Jul-Aug;6(4):277–280. doi: 10.1016/0741-8329(89)90083-9. [DOI] [PubMed] [Google Scholar]
  10. Bunce K., Tyers M., Beranek P. Clinical evaluation of 5-HT3 receptor antagonists as anti-emetics. Trends Pharmacol Sci. 1991 Feb;12(2):46–48. doi: 10.1016/0165-6147(91)90493-c. [DOI] [PubMed] [Google Scholar]
  11. Butler M. O., Morinobu S., Duman R. S. Chronic electroconvulsive seizures increase the expression of serotonin2 receptor mRNA in rat frontal cortex. J Neurochem. 1993 Oct;61(4):1270–1276. doi: 10.1111/j.1471-4159.1993.tb13618.x. [DOI] [PubMed] [Google Scholar]
  12. Canton H., Verrièle L., Colpaert F. C. Binding of typical and atypical antipsychotics to 5-HT1C and 5-HT2 sites: clozapine potently interacts with 5-HT1C sites. Eur J Pharmacol. 1990 Nov 20;191(1):93–96. doi: 10.1016/0014-2999(90)94100-c. [DOI] [PubMed] [Google Scholar]
  13. Carboni E., Acquas E., Frau R., Di Chiara G. Differential inhibitory effects of a 5-HT3 antagonist on drug-induced stimulation of dopamine release. Eur J Pharmacol. 1989 May 30;164(3):515–519. doi: 10.1016/0014-2999(89)90259-8. [DOI] [PubMed] [Google Scholar]
  14. Cheetham S. C., Crompton M. R., Katona C. L., Horton R. W. Brain 5-HT2 receptor binding sites in depressed suicide victims. Brain Res. 1988 Mar 8;443(1-2):272–280. doi: 10.1016/0006-8993(88)91621-6. [DOI] [PubMed] [Google Scholar]
  15. Cheng A. V., Ferrier I. N., Morris C. M., Jabeen S., Sahgal A., McKeith I. G., Edwardson J. A., Perry R. H., Perry E. K. Cortical serotonin-S2 receptor binding in Lewy body dementia, Alzheimer's and Parkinson's diseases. J Neurol Sci. 1991 Nov;106(1):50–55. doi: 10.1016/0022-510x(91)90193-b. [DOI] [PubMed] [Google Scholar]
  16. Closse A. [3H]Mesulergine, a selective ligand for serotonin-2 receptors. Life Sci. 1983 May 23;32(21):2485–2495. doi: 10.1016/0024-3205(83)90375-2. [DOI] [PubMed] [Google Scholar]
  17. Conn P. J., Janowsky A., Sanders-Bush E. Denervation supersensitivity of 5-HT-1c receptors in rat choroid plexus. Brain Res. 1987 Jan 6;400(2):396–398. doi: 10.1016/0006-8993(87)90641-x. [DOI] [PubMed] [Google Scholar]
  18. Conn P. J., Sanders-Bush E. Central serotonin receptors: effector systems, physiological roles and regulation. Psychopharmacology (Berl) 1987;92(3):267–277. doi: 10.1007/BF00210830. [DOI] [PubMed] [Google Scholar]
  19. Conn P. J., Sanders-Bush E. Regulation of serotonin-stimulated phosphoinositide hydrolysis: relation to the serotonin 5-HT-2 binding site. J Neurosci. 1986 Dec;6(12):3669–3675. doi: 10.1523/JNEUROSCI.06-12-03669.1986. [DOI] [PMC free article] [PubMed] [Google Scholar]
  20. Cowen P. J., Charig E. M., Fraser S., Elliott J. M. Platelet 5-HT receptor binding during depressive illness and tricyclic antidepressant treatment. J Affect Disord. 1987 Jul-Aug;13(1):45–50. doi: 10.1016/0165-0327(87)90072-3. [DOI] [PubMed] [Google Scholar]
  21. De Clerck F., Xhonneux B., Leysen J., Janssen P. A. Evidence for functional 5-HT2 receptor sites on human blood platelets. Biochem Pharmacol. 1984 Sep 1;33(17):2807–2811. doi: 10.1016/0006-2952(84)90699-3. [DOI] [PubMed] [Google Scholar]
  22. Derkach V., Surprenant A., North R. A. 5-HT3 receptors are membrane ion channels. Nature. 1989 Jun 29;339(6227):706–709. doi: 10.1038/339706a0. [DOI] [PubMed] [Google Scholar]
  23. Edwards E., Harkins K., Ashby C. R., Jr, Wang R. Y. Effect of 5-hydroxytryptamine3 receptor agonists on phosphoinositides hydrolysis in the rat fronto-cingulate and entorhinal cortices. J Pharmacol Exp Ther. 1991 Mar;256(3):1025–1032. [PubMed] [Google Scholar]
  24. Gold P. W., Goodwin F. K., Chrousos G. P. Clinical and biochemical manifestations of depression. Relation to the neurobiology of stress (2) N Engl J Med. 1988 Aug 18;319(7):413–420. doi: 10.1056/NEJM198808183190706. [DOI] [PubMed] [Google Scholar]
  25. Green A. R. Evolving concepts on the interactions between antidepressant treatments and monoamine neurotransmitters. Neuropharmacology. 1987 Jul;26(7B):815–822. doi: 10.1016/0028-3908(87)90057-8. [DOI] [PubMed] [Google Scholar]
  26. Hamon M., Lanfumey L., el Mestikawy S., Boni C., Miquel M. C., Bolaños F., Schechter L., Gozlan H. The main features of central 5-HT1 receptors. Neuropsychopharmacology. 1990 Oct-Dec;3(5-6):349–360. [PubMed] [Google Scholar]
  27. Hamon M., Mallat M., Herbet A., Nelson D. L., Audinot M., Pichat L., Glowinski J. [3H]Metergoline: a new ligand of serotonin receptors in the rat brain. J Neurochem. 1981 Feb;36(2):613–626. doi: 10.1111/j.1471-4159.1981.tb01634.x. [DOI] [PubMed] [Google Scholar]
  28. Hartig P. R., Kadan M. J., Evans M. J., Krohn A. M. 125I-LSD: a high sensitivity ligand for serotonin receptors. Eur J Pharmacol. 1983 May 6;89(3-4):321–322. doi: 10.1016/0014-2999(83)90515-0. [DOI] [PubMed] [Google Scholar]
  29. Hartig P., Kao H. T., Macchi M., Adham N., Zgombick J., Weinshank R., Branchek T. The molecular biology of serotonin receptors. An overview. Neuropsychopharmacology. 1990 Oct-Dec;3(5-6):335–347. [PubMed] [Google Scholar]
  30. Hoyer D., Clarke D. E., Fozard J. R., Hartig P. R., Martin G. R., Mylecharane E. J., Saxena P. R., Humphrey P. P. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev. 1994 Jun;46(2):157–203. [PubMed] [Google Scholar]
  31. Hoyer D., Pazos A., Probst A., Palacios J. M. Serotonin receptors in the human brain. II. Characterization and autoradiographic localization of 5-HT1C and 5-HT2 recognition sites. Brain Res. 1986 Jun 18;376(1):97–107. doi: 10.1016/0006-8993(86)90903-0. [DOI] [PubMed] [Google Scholar]
  32. Hrdina P. D., Demeter E., Vu T. B., Sótónyi P., Palkovits M. 5-HT uptake sites and 5-HT2 receptors in brain of antidepressant-free suicide victims/depressives: increase in 5-HT2 sites in cortex and amygdala. Brain Res. 1993 Jun 18;614(1-2):37–44. doi: 10.1016/0006-8993(93)91015-k. [DOI] [PubMed] [Google Scholar]
  33. Hrdina P. D., Vu T. B. Chronic fluoxetine treatment upregulates 5-HT uptake sites and 5-HT2 receptors in rat brain: an autoradiographic study. Synapse. 1993 Aug;14(4):324–331. doi: 10.1002/syn.890140410. [DOI] [PubMed] [Google Scholar]
  34. Iqbal N., Asnis G. M., Wetzler S., Kay S. R., van Praag H. M. The role of serotonin in schizophrenia. New findings. Schizophr Res. 1991 Sep;5(2):181–182. doi: 10.1016/0920-9964(91)90046-t. [DOI] [PubMed] [Google Scholar]
  35. Jones A. L., Hill A. S., Soukop M., Hutcheon A. W., Cassidy J., Kaye S. B., Sikora K., Carney D. N., Cunningham D. Comparison of dexamethasone and ondansetron in the prophylaxis of emesis induced by moderately emetogenic chemotherapy. Lancet. 1991 Aug 24;338(8765):483–487. doi: 10.1016/0140-6736(91)90554-3. [DOI] [PubMed] [Google Scholar]
  36. Jones B. J., Costall B., Domeney A. M., Kelly M. E., Naylor R. J., Oakley N. R., Tyers M. B. The potential anxiolytic activity of GR38032F, a 5-HT3-receptor antagonist. Br J Pharmacol. 1988 Apr;93(4):985–993. doi: 10.1111/j.1476-5381.1988.tb11489.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  37. Joyce J. N., Shane A., Lexow N., Winokur A., Casanova M. F., Kleinman J. E. Serotonin uptake sites and serotonin receptors are altered in the limbic system of schizophrenics. Neuropsychopharmacology. 1993 Jun;8(4):315–336. doi: 10.1038/npp.1993.32. [DOI] [PubMed] [Google Scholar]
  38. Julius D., Huang K. N., Livelli T. J., Axel R., Jessell T. M. The 5HT2 receptor defines a family of structurally distinct but functionally conserved serotonin receptors. Proc Natl Acad Sci U S A. 1990 Feb;87(3):928–932. doi: 10.1073/pnas.87.3.928. [DOI] [PMC free article] [PubMed] [Google Scholar]
  39. Julius D., MacDermott A. B., Axel R., Jessell T. M. Molecular characterization of a functional cDNA encoding the serotonin 1c receptor. Science. 1988 Jul 29;241(4865):558–564. doi: 10.1126/science.3399891. [DOI] [PubMed] [Google Scholar]
  40. Kendall D. A., Nahorski S. R. 5-Hydroxytryptamine-stimulated inositol phospholipid hydrolysis in rat cerebral cortex slices: pharmacological characterization and effects of antidepressants. J Pharmacol Exp Ther. 1985 May;233(2):473–479. [PubMed] [Google Scholar]
  41. Kilpatrick G. J., Jones B. J., Tyers M. B. Identification and distribution of 5-HT3 receptors in rat brain using radioligand binding. Nature. 1987 Dec 24;330(6150):746–748. doi: 10.1038/330746a0. [DOI] [PubMed] [Google Scholar]
  42. Klimek V., Zak-Knapik J., Mackowiak M. Effects of repeated treatment with fluoxetine and citalopram, 5-HT uptake inhibitors, on 5-HT1A and 5-HT2 receptors in the rat brain. J Psychiatry Neurosci. 1994 Jan;19(1):63–67. [PMC free article] [PubMed] [Google Scholar]
  43. Kuoppamäki M., Seppälä T., Syvälahti E., Hietala J. Chronic clozapine treatment decreases 5-hydroxytryptamine1C receptor density in the rat choroid plexus: comparison with haloperidol. J Pharmacol Exp Ther. 1993 Mar;264(3):1262–1267. [PubMed] [Google Scholar]
  44. Kuroda Y., Mikuni M., Ogawa T., Takahashi K. Effect of ACTH, adrenalectomy and the combination treatment on the density of 5-HT2 receptor binding sites in neocortex of rat forebrain and 5-HT2 receptor-mediated wet-dog shake behaviors. Psychopharmacology (Berl) 1992;108(1-2):27–32. doi: 10.1007/BF02245281. [DOI] [PubMed] [Google Scholar]
  45. Kusumi I., Koyama T., Yamashita I. Serotonin-stimulated Ca2+ response is increased in the blood platelets of depressed patients. Biol Psychiatry. 1991 Aug 1;30(3):310–312. doi: 10.1016/0006-3223(91)90114-2. [DOI] [PubMed] [Google Scholar]
  46. Lal H., Prather P. L., Rezazadeh S. M. Potential role of 5HT1C and/or 5HT2 receptors in the mianserin-induced prevention of anxiogenic behaviors occurring during ethanol withdrawal. Alcohol Clin Exp Res. 1993 Apr;17(2):411–417. doi: 10.1111/j.1530-0277.1993.tb00785.x. [DOI] [PubMed] [Google Scholar]
  47. Lee M. A., Meltzer H. Y. Neuroendocrine responses to serotonergic agents in alcoholics. Biol Psychiatry. 1991 Nov 15;30(10):1017–1030. doi: 10.1016/0006-3223(91)90122-3. [DOI] [PubMed] [Google Scholar]
  48. Lesch K. P., Wolozin B. L., Estler H. C., Murphy D. L., Riederer P. Isolation of a cDNA encoding the human brain serotonin transporter. J Neural Transm Gen Sect. 1993;91(1):67–72. doi: 10.1007/BF01244919. [DOI] [PubMed] [Google Scholar]
  49. Lesch K. P., Wolozin B. L., Murphy D. L., Reiderer P. Primary structure of the human platelet serotonin uptake site: identity with the brain serotonin transporter. J Neurochem. 1993 Jun;60(6):2319–2322. doi: 10.1111/j.1471-4159.1993.tb03522.x. [DOI] [PubMed] [Google Scholar]
  50. Levy A. D., Van de Kar L. D. Endocrine and receptor pharmacology of serotonergic anxiolytics, antipsychotics and antidepressants. Life Sci. 1992;51(2):83–94. doi: 10.1016/0024-3205(92)90001-6. [DOI] [PubMed] [Google Scholar]
  51. Leysen J. E., Niemegeers C. J., Tollenaere J. P., Laduron P. M. Serotonergic component of neuroleptic receptors. Nature. 1978 Mar 9;272(5649):168–171. doi: 10.1038/272168a0. [DOI] [PubMed] [Google Scholar]
  52. Leysen J. E., Niemegeers C. J., Van Nueten J. M., Laduron P. M. [3H]Ketanserin (R 41 468), a selective 3H-ligand for serotonin2 receptor binding sites. Binding properties, brain distribution, and functional role. Mol Pharmacol. 1982 Mar;21(2):301–314. [PubMed] [Google Scholar]
  53. Lieberman J. A., Koreen A. R. Neurochemistry and neuroendocrinology of schizophrenia: a selective review. Schizophr Bull. 1993;19(2):371–429. doi: 10.1093/schbul/19.2.371. [DOI] [PubMed] [Google Scholar]
  54. Loric S., Launay J. M., Colas J. F., Maroteaux L. New mouse 5-HT2-like receptor. Expression in brain, heart and intestine. FEBS Lett. 1992 Nov 9;312(2-3):203–207. doi: 10.1016/0014-5793(92)80936-b. [DOI] [PubMed] [Google Scholar]
  55. Lovinger D. M., White G. Ethanol potentiation of 5-hydroxytryptamine3 receptor-mediated ion current in neuroblastoma cells and isolated adult mammalian neurons. Mol Pharmacol. 1991 Aug;40(2):263–270. [PubMed] [Google Scholar]
  56. Mann J. J., Stanley M., McBride P. A., McEwen B. S. Increased serotonin2 and beta-adrenergic receptor binding in the frontal cortices of suicide victims. Arch Gen Psychiatry. 1986 Oct;43(10):954–959. doi: 10.1001/archpsyc.1986.01800100048007. [DOI] [PubMed] [Google Scholar]
  57. Maricq A. V., Peterson A. S., Brake A. J., Myers R. M., Julius D. Primary structure and functional expression of the 5HT3 receptor, a serotonin-gated ion channel. Science. 1991 Oct 18;254(5030):432–437. doi: 10.1126/science.1718042. [DOI] [PubMed] [Google Scholar]
  58. Martin G. R., Humphrey P. P. Receptors for 5-hydroxytryptamine: current perspectives on classification and nomenclature. Neuropharmacology. 1994 Mar-Apr;33(3-4):261–273. doi: 10.1016/0028-3908(94)90058-2. [DOI] [PubMed] [Google Scholar]
  59. McElroy S. L., Dessain E. C., Pope H. G., Jr, Cole J. O., Keck P. E., Jr, Frankenberg F. R., Aizley H. G., O'Brien S. Clozapine in the treatment of psychotic mood disorders, schizoaffective disorder, and schizophrenia. J Clin Psychiatry. 1991 Oct;52(10):411–414. [PubMed] [Google Scholar]
  60. McKenna D. J., Peroutka S. J. Differentiation of 5-hydroxytryptamine2 receptor subtypes using 125I-R-(-)2,5-dimethoxy-4-iodo-phenylisopropylamine and 3H-ketanserin. J Neurosci. 1989 Oct;9(10):3482–3490. doi: 10.1523/JNEUROSCI.09-10-03482.1989. [DOI] [PMC free article] [PubMed] [Google Scholar]
  61. Meltzer H. Y. Clinical studies on the mechanism of action of clozapine: the dopamine-serotonin hypothesis of schizophrenia. Psychopharmacology (Berl) 1989;99 (Suppl):S18–S27. doi: 10.1007/BF00442554. [DOI] [PubMed] [Google Scholar]
  62. Mikuni M., Kusumi I., Kagaya A., Kuroda Y., Mori H., Takahashi K. Increased 5-HT-2 receptor function as measured by serotonin-stimulated phosphoinositide hydrolysis in platelets of depressed patients. Prog Neuropsychopharmacol Biol Psychiatry. 1991;15(1):49–61. doi: 10.1016/0278-5846(91)90040-8. [DOI] [PubMed] [Google Scholar]
  63. Milne R. J., Heel R. C. Ondansetron. Therapeutic use as an antiemetic. Drugs. 1991 Apr;41(4):574–595. doi: 10.2165/00003495-199141040-00006. [DOI] [PubMed] [Google Scholar]
  64. Mita T., Hanada S., Nishino N., Kuno T., Nakai H., Yamadori T., Mizoi Y., Tanaka C. Decreased serotonin S2 and increased dopamine D2 receptors in chronic schizophrenics. Biol Psychiatry. 1986 Dec;21(14):1407–1414. doi: 10.1016/0006-3223(86)90332-x. [DOI] [PubMed] [Google Scholar]
  65. Mizuta T., Segawa T. Chronic effects of imipramine and lithium on 5-HT receptor subtypes in rat frontal cortex, hippocampus and choroid plexus: quantitative receptor autoradiographic analysis. Jpn J Pharmacol. 1989 Jul;50(3):315–326. doi: 10.1254/jjp.50.315. [DOI] [PubMed] [Google Scholar]
  66. Mizuta T., Segawa T. Chronic effects of imipramine and lithium on postsynaptic 5-HT1A and 5-HT1B sites and on presynaptic 5-HT3 sites in rat brain. Jpn J Pharmacol. 1988 Jun;47(2):107–113. doi: 10.1254/jjp.47.107. [DOI] [PubMed] [Google Scholar]
  67. Molineaux S. M., Jessell T. M., Axel R., Julius D. 5-HT1c receptor is a prominent serotonin receptor subtype in the central nervous system. Proc Natl Acad Sci U S A. 1989 Sep;86(17):6793–6797. doi: 10.1073/pnas.86.17.6793. [DOI] [PMC free article] [PubMed] [Google Scholar]
  68. Molliver M. E. Serotonergic neuronal systems: what their anatomic organization tells us about function. J Clin Psychopharmacol. 1987 Dec;7(6 Suppl):3S–23S. [PubMed] [Google Scholar]
  69. Owen F., Cross A. J., Crow T. J., Deakin J. F., Ferrier I. N., Lofthouse R., Poulter M. Brain 5-HT-2 receptors and suicide. Lancet. 1983 Nov 26;2(8361):1256–1256. doi: 10.1016/s0140-6736(83)91310-7. [DOI] [PubMed] [Google Scholar]
  70. Pandey G. N., Pandey S. C., Isaac L., Davis J. M. Effect of electroconvulsive shock on 5-HT2 and alpha 1-adrenoceptors and phosphoinositide signalling system in rat brain. Eur J Pharmacol. 1992 Aug 3;226(4):303–310. doi: 10.1016/0922-4106(92)90047-y. [DOI] [PubMed] [Google Scholar]
  71. Pandey G. N., Pandey S. C., Janicak P. G., Marks R. C., Davis J. M. Platelet serotonin-2 receptor binding sites in depression and suicide. Biol Psychiatry. 1990 Aug 1;28(3):215–222. doi: 10.1016/0006-3223(90)90576-n. [DOI] [PubMed] [Google Scholar]
  72. Pandey S. C., Dubey M. P., Piano M. R., Schwertz D. W., Davis J. M., Pandey G. N. Modulation of 5-HT1C receptors and phosphoinositide system by ethanol consumption in rat brain and choroid plexus. Eur J Pharmacol. 1993 Sep 15;247(1):81–88. doi: 10.1016/0922-4106(93)90140-5. [DOI] [PubMed] [Google Scholar]
  73. Pandey S. C., Kim S. W., Davis J. M., Pandey G. N. Platelet serotonin-2 receptors in obsessive-compulsive disorder. Biol Psychiatry. 1993 Mar 1;33(5):367–372. doi: 10.1016/0006-3223(93)90326-9. [DOI] [PubMed] [Google Scholar]
  74. Pandey S. C., Piano M. R., Schwertz D. W., Davis J. M., Pandey G. N. Effect of ethanol administration and withdrawal on serotonin receptor subtypes and receptor-mediated phosphoinositide hydrolysis in rat brain. Alcohol Clin Exp Res. 1992 Dec;16(6):1110–1116. doi: 10.1111/j.1530-0277.1992.tb00706.x. [DOI] [PubMed] [Google Scholar]
  75. Pandey S. C., Sharma R. P., Janicak P. G., Marks R. C., Davis J. M., Pandey G. N. Platelet serotonin-2 receptors in schizophrenia: effects of illness and neuroleptic treatment. Psychiatry Res. 1993 Jul;48(1):57–68. doi: 10.1016/0165-1781(93)90113-u. [DOI] [PubMed] [Google Scholar]
  76. Paul S. M., Rehavi M., Skolnick P., Ballenger J. C., Goodwin F. K. Depressed patients have decreased binding of tritiated imipramine to platelet serotonin "transporter". Arch Gen Psychiatry. 1981 Dec;38(12):1315–1317. doi: 10.1001/archpsyc.1981.01780370017001. [DOI] [PubMed] [Google Scholar]
  77. Pazos A., Cortés R., Palacios J. M. Quantitative autoradiographic mapping of serotonin receptors in the rat brain. II. Serotonin-2 receptors. Brain Res. 1985 Nov 4;346(2):231–249. doi: 10.1016/0006-8993(85)90857-1. [DOI] [PubMed] [Google Scholar]
  78. Peroutka S. J. 5-Hydroxytryptamine receptor subtypes: molecular, biochemical and physiological characterization. Trends Neurosci. 1988 Nov;11(11):496–500. doi: 10.1016/0166-2236(88)90011-2. [DOI] [PubMed] [Google Scholar]
  79. Peroutka S. J., Hamik A. [3H]quipazine labels 5-HT3 recognition sites in rat cortical membranes. Eur J Pharmacol. 1988 Mar 29;148(2):297–299. doi: 10.1016/0014-2999(88)90579-1. [DOI] [PubMed] [Google Scholar]
  80. Peroutka S. J. Serotonin receptor subtypes and neuropsychiatric diseases: focus on 5-HT1D and 5-HT3 receptor agents. Pharmacol Rev. 1991 Dec;43(4):579–586. [PubMed] [Google Scholar]
  81. Peroutka S. J., Snyder S. H. [3H]Mianserin: differential labeling of serotonin and histamine receptors in rat brain. J Pharmacol Exp Ther. 1981 Jan;216(1):142–148. [PubMed] [Google Scholar]
  82. Peroutka S. J., Synder S. H. Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency. Am J Psychiatry. 1980 Dec;137(12):1518–1522. doi: 10.1176/ajp.137.12.1518. [DOI] [PubMed] [Google Scholar]
  83. Pritchett D. B., Bach A. W., Wozny M., Taleb O., Dal Toso R., Shih J. C., Seeburg P. H. Structure and functional expression of cloned rat serotonin 5HT-2 receptor. EMBO J. 1988 Dec 20;7(13):4135–4140. doi: 10.1002/j.1460-2075.1988.tb03308.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  84. Roth B. L., Ciaranello R. D. Chronic mianserin treatment decreases 5-HT2 receptor binding without altering 5-HT2 receptor mRNA levels. Eur J Pharmacol. 1991 Jun 19;207(2):169–172. doi: 10.1016/0922-4106(91)90093-w. [DOI] [PubMed] [Google Scholar]
  85. Roth B. L., Hamblin M. W., Ciaranello R. D. Developmental regulation of 5-HT2 and 5-HT1c mRNA and receptor levels. Brain Res Dev Brain Res. 1991 Jan 15;58(1):51–58. doi: 10.1016/0165-3806(91)90236-c. [DOI] [PubMed] [Google Scholar]
  86. Roy A. Genetics of suicide. Ann N Y Acad Sci. 1986;487:97–105. doi: 10.1111/j.1749-6632.1986.tb27889.x. [DOI] [PubMed] [Google Scholar]
  87. Sanders-Bush E. Adaptive regulation of central serotonin receptors linked to phosphoinositide hydrolysis. Neuropsychopharmacology. 1990 Oct-Dec;3(5-6):411–416. [PubMed] [Google Scholar]
  88. Sanders-Bush E., Breeding M., Knoth K., Tsutsumi M. Sertraline-induced desensitization of the serotonin 5HT-2 receptor transmembrane signaling system. Psychopharmacology (Berl) 1989;99(1):64–69. doi: 10.1007/BF00634454. [DOI] [PubMed] [Google Scholar]
  89. Sanders-Bush E., Breeding M. Putative selective 5-HT-2 antagonists block serotonin 5-HT-1c receptors in the choroid plexus. J Pharmacol Exp Ther. 1988 Oct;247(1):169–173. [PubMed] [Google Scholar]
  90. Sanders-Bush E., Tsutsumi M., Burris K. D. Serotonin receptors and phosphatidylinositol turnover. Ann N Y Acad Sci. 1990;600:224–236. doi: 10.1111/j.1749-6632.1990.tb16885.x. [DOI] [PubMed] [Google Scholar]
  91. Sanna E., Dildy-Mayfield J. E., Harris R. A. Ethanol inhibits the function of 5-hydroxytryptamine type 1c and muscarinic M1 G protein-linked receptors in Xenopus oocytes expressing brain mRNA: role of protein kinase C. Mol Pharmacol. 1994 May;45(5):1004–1012. [PubMed] [Google Scholar]
  92. Schmidt A. W., Peroutka S. J. 5-Hydroxytryptamine receptor "families". FASEB J. 1989 Sep;3(11):2242–2249. doi: 10.1096/fasebj.3.11.2673898. [DOI] [PubMed] [Google Scholar]
  93. Schächter M., Geaney D. P., Grahame-Smith D. G., Cowen P. J., Elliott J. M. Increased platelet membrane [3H]-LSD binding in patients on chronic neuroleptic treatment. Br J Clin Pharmacol. 1985 Apr;19(4):453–457. doi: 10.1111/j.1365-2125.1985.tb02670.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  94. Sellers E. M., Higgins G. A., Sobell M. B. 5-HT and alcohol abuse. Trends Pharmacol Sci. 1992 Feb;13(2):69–75. doi: 10.1016/0165-6147(92)90026-3. [DOI] [PubMed] [Google Scholar]
  95. Simonsson P., Alling C. The 5-hydroxytryptamine stimulated formation of inositol phosphate is inhibited in platelets from alcoholics. Life Sci. 1988;42(4):385–391. doi: 10.1016/0024-3205(88)90076-8. [DOI] [PubMed] [Google Scholar]
  96. Spurlock G., Buckland P., O'Donovan M., McGuffin P. Lack of effect of antidepressant drugs on the levels of mRNAs encoding serotonergic receptors, synthetic enzymes and 5HT transporter. Neuropharmacology. 1994 Mar-Apr;33(3-4):433–440. doi: 10.1016/0028-3908(94)90073-6. [DOI] [PubMed] [Google Scholar]
  97. Stanley M., Mann J. J. Increased serotonin-2 binding sites in frontal cortex of suicide victims. Lancet. 1983 Jan 29;1(8318):214–216. doi: 10.1016/s0140-6736(83)92590-4. [DOI] [PubMed] [Google Scholar]
  98. Stanley M., Virgilio J., Gershon S. Tritiated imipramine binding sites are decreased in the frontal cortex of suicides. Science. 1982 Jun 18;216(4552):1337–1339. doi: 10.1126/science.7079769. [DOI] [PubMed] [Google Scholar]
  99. Stockmeier C. A., Kellar K. J. In vivo regulation of the serotonin-2 receptor in rat brain. Life Sci. 1986 Jan 13;38(2):117–127. doi: 10.1016/0024-3205(86)90003-2. [DOI] [PubMed] [Google Scholar]
  100. Tajuddin N., Druse M. J. Effects of in utero ethanol exposure on cortical 5-HT2 binding sites. Alcohol. 1988 Nov-Dec;5(6):461–464. doi: 10.1016/0741-8329(88)90083-3. [DOI] [PubMed] [Google Scholar]
  101. Tecott L. H., Maricq A. V., Julius D. Nervous system distribution of the serotonin 5-HT3 receptor mRNA. Proc Natl Acad Sci U S A. 1993 Feb 15;90(4):1430–1434. doi: 10.1073/pnas.90.4.1430. [DOI] [PMC free article] [PubMed] [Google Scholar]
  102. Titeler M., Lyon R. A., Davis K. H., Glennon R. A. Selectivity of serotonergic drugs for multiple brain serotonin receptors. Role of [3H]-4-bromo-2,5-dimethoxyphenylisopropylamine ([3H]DOB), a 5-HT2 agonist radioligand. Biochem Pharmacol. 1987 Oct 1;36(19):3265–3271. doi: 10.1016/0006-2952(87)90643-5. [DOI] [PubMed] [Google Scholar]
  103. Ulrichsen J. Alterations in serotonin receptor subtypes in ethanol-dependent rats. Alcohol Alcohol. 1991;26(5-6):567–573. doi: 10.1093/oxfordjournals.alcalc.a045160. [DOI] [PubMed] [Google Scholar]
  104. Vetulani J., Lebrecht U., Pilc A. Enhancement of responsiveness of the central serotonergic system and serotonin-2 receptor density in rat frontal cortex by electroconvulsive treatment. Eur J Pharmacol. 1981 Nov 19;76(1):81–85. doi: 10.1016/0014-2999(81)90012-1. [DOI] [PubMed] [Google Scholar]
  105. Whitaker P. M., Crow T. J., Ferrier I. N. Tritiated LSD binding in frontal cortex in schizophrenia. Arch Gen Psychiatry. 1981 Mar;38(3):278–280. doi: 10.1001/archpsyc.1981.01780280046004. [DOI] [PubMed] [Google Scholar]
  106. Wong D. T., Robertson D. W., Reid L. R. Specific [3H]LY278584 binding to 5-HT3 recognition sites in rat cerebral cortex. Eur J Pharmacol. 1989 Jul 4;166(1):107–110. doi: 10.1016/0014-2999(89)90689-4. [DOI] [PubMed] [Google Scholar]
  107. Yagaloff K. A., Hartig P. R. 125I-lysergic acid diethylamide binds to a novel serotonergic site on rat choroid plexus epithelial cells. J Neurosci. 1985 Dec;5(12):3178–3183. doi: 10.1523/JNEUROSCI.05-12-03178.1985. [DOI] [PMC free article] [PubMed] [Google Scholar]
  108. Yates M., Leake A., Candy J. M., Fairbairn A. F., McKeith I. G., Ferrier I. N. 5HT2 receptor changes in major depression. Biol Psychiatry. 1990 Mar 1;27(5):489–496. doi: 10.1016/0006-3223(90)90440-d. [DOI] [PubMed] [Google Scholar]
  109. Zifa E., Fillion G. 5-Hydroxytryptamine receptors. Pharmacol Rev. 1992 Sep;44(3):401–458. [PubMed] [Google Scholar]
  110. de Chaffoy de Courcelles D., Leysen J. E., De Clerck F., Van Belle H., Janssen P. A. Evidence that phospholipid turnover is the signal transducing system coupled to serotonin-S2 receptor sites. J Biol Chem. 1985 Jun 25;260(12):7603–7608. [PubMed] [Google Scholar]

Articles from Journal of Psychiatry and Neuroscience are provided here courtesy of Canadian Science Publishing

RESOURCES