Activation is hallucinogenic and antagonism is therapeutic: Role of 5- HT(2A) receptors in atypical antipsychotic drug actions

Neuroscientist

Volumn 5, Issue 4, 1999, Pages 254-262

  Roth, Bryan L ^a   Willins, David L ^a   Kristiansen, Kurt ^a   Kroeze, Wesley K ^a  

^a CASE WESTERN RESERVE UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

5 HT(2A) receptors; Atypical antipsychotic drugs; Clozapine; Serotonin

Indexed keywords

ALPHA (2,3 DIMETHOXYPHENYL) 1 [2 (4 FLUOROPHENYL)ETHYL] 4 PIPERIDINEMETHANOL; BROLAMFETAMINE; CLOZAPINE; FLUPERLAPINE; NEUROLEPTIC AGENT; PSYCHEDELIC AGENT; SEROTONIN 2A RECEPTOR;

DRUG RECEPTOR BINDING; DRUG TARGETING; HALLUCINATION; HUMAN; INTERNALIZATION; MOLECULAR INTERACTION; RECEPTOR AFFINITY; RECEPTOR UPREGULATION; REVIEW; THERMODYNAMICS;

EID: 0032811255     PISSN: 10738584     EISSN: None     Source Type: Journal    
DOI: 10.1177/107385849900500414     Document Type: Review

References (61)

1. Wooley DW, Shaw E. A biochemical and pharmacological suggestion about certain mental disorders. Proc Natl Acad Sci U S A 1954;40:228-31.
2. Hollister LE. Drug-induced psychoses and schizophrenic reactions, a critical comparison. Ann NY Acad Sci 1962;96:80-8.
3. Roth BL, Meltzer H. The role of serotonin in schizophrenia, in Bloom F, Kupfer D, editors. Psychopharmacology: the fourth generation of progress. New York: Raven Press; 1995. p. 1215-27.
4. Aldous FAB, Barrass BC, Brewster K, Buxton DA, Green DA, Pinder RM, et al. Structure-activity relationships in psychotomimetic phenylalkylamines. J Med Chem 1974;17:1100-11.
5. Knoll J, Vizi ES, Knoll B. Pharmacological studies on parabromo-methamphetamine (V-111) and LSD. Acta Physiol Acad Sci Hung 1970;37:151-70.
6. Glennon RA, Young R, Rosencrans JA. Antagonism of the effects of the hallucinogen DOM, and the purported 5-HT agonist quipazine, by 5-HT2 antagonists. Eur J Pharmacol 1983;91:189-93.
7. Glennon RA. Do classical hallucinogens act as 5-HT2 agonists or antagonists? Neuropsychopharmacol 1990;3:509-17.
8. Burris KD, Breeding M, Sanders-Bush E. (+)Lysergic acid diethylamide, but not its nonhallucinogenic congeners, is a potent serotonin 5HT1c receptor agonist. J Pharmacol Exp Ther 1991; 258:891-6.
9. Ismaiel AM, De Los Angeles J, Teitler M, Ingher S, Glennon RA. Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2-versus 5-HT1C-selective antagonist. J Med Chem 1993;36:2519-25.
10. 2A receptors. Mol Pharmacol 1997;52:259-66.
11. 2A receptors: ergolines require an aromatic residue at position 340 for high affinity binding. Mol Pharmacol 1995;47:450-7.
12. 3H]ketanserin binding to 5-hydroxytryptamine2 receptors. Mol Pharmacol 1993;47:755-61.
13. 2A receptor. Ser3.36(159) provides a second interaction site for the protonated amine of serotonin but not of lysergic acid diethylamide or bufotenin. J Biol Chem 1996;271:14672-5.
14. 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines. Mol Pharmacol 1994;45:277-86.
15. 2 receptor subtypes. Mol Pharmacol 1990; 38:594-8.
16. 2A receptors: evidence in favor of a modified ternary complex model. J Pharmacol Exp Ther 1997;280:576-83.
17. 2A antagonists. Soc Neurosci Abstr 1996;22:1778.
18. 2C receptor. J Neurochem 1997;69:1138-44.
19. 2A receptor. J Biol Chem 1995;270:16683-8.
20. Lefkowitz R, Coteccdhia S, Samama P, Costa T. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci 1993;14:303-7.
21. Altar CA, Wasley AM, Neale RF, Stone GA. Typical and atypical antipsychotic occupancy of D2 and S2 receptors: an autoradiographic analysis in rat brain. Brain Res Bull 1986;16:517-25.
22. Rasmussen K, Aghajanian GK. Potency of antipsychotics in reversing the effects of a hallucinogenic drug on locus coeruleus neurons correlates with 5-HT2 binding affinity. Neuropsychopharmacol 1988;1:101-7.
23. i values. J Pharmacol Exp Ther 1989;251:238-46
24. Fischer-Cornelssen KA. Fluperlapine in 104 schizophrenic patients. Open multicenter trial. Arzneimittelforschung, 1984;34: 125-30.
25. Woggon B, Beckman H, Heinrich K, Linden E, Krebs E, Kufferel B, et al. Clinically relevant differences in the therapeutic profile of fluperlapine compared to haloperidol in the treatment of schizophrenic psychosis: results of a multicenter double-blind study. Pharmacopsych 1986;19:204-5.
26. Roth BL, Ciaranello RD, Meltzer HY. Binding of typical and atypical antipsychotic agents to transiently expressed 5-HT1C receptors. J Pharmacol Exp Ther 1992;260:1361-5.
27. Roth BL, Craigo SC, Choudhary MS, Uluer A, Monsma FJ Jr, Shen Y, et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther 1994;268:1403-10.
28. Roth BL, Meltzer H, Khan N. Binding of typical and atypical antipsychotic drugs to multiple neurotransmitter receptors. Adv Pharmacol 1998;42:482-5.
29. 6 serotonin receptor. J Neurochem 1996;66:47-56.
30. Roth BL, Tandra S, Burgess LH, Sibley DR, Meltzer HY. D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs. Psychopharmacology (Berl) 1995;120:365-8.
31. 6 serotonin receptors may reflect psychoactive profile. Mol Med 1995;1:398-406.
32. Sorensen SM, Kehne JH, Fadayel GM, Humphreys TM, Ketteler HJ, Sullivan CK, et al. Characterization of the 5-HT2 antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies. J Pharmacol Exp Ther 1993;266:684-91.
33. Mizuki Y, Kajimura N, Imai T, Suetsugi M, Kai S, Kaneyuki H, et al. Effects of mianserin on negative symptoms in schizophrenia. Int Clin Psychopharmacol 1990;5:83-95.
34. Duinkerke SJ, Botter PA, Jansen AA, van Dongen PA, van Haaften AJ, Boom AJ, et al. Ritanserin, a selective 5-HT2/1C antagonist, and negative symptoms in schizophrenia. A placebo-controlled double-blind trial. Br J Psychiatry 1993;163:451-5.
35. Araneda R, Andrade R. 5-Hydroxytryptamine2 and 5-hydroxytryptaminelA receptors mediate opposing responses on membrane excitability in rat association cortex. Neurosci 1991;40:399-412.
36. Aghajanian GK, Marek GJ. Serotonin induces excitatory postsynaptic potentials in apical dendrites of neocortical pyramidal cells. Neuropharmacol 1997;36:589-99.
37. 2A receptors are expressed on pyramidal cells and interneurons in the rat cortex. Synapse 1997;27:79-82.
38. 2C receptors. Brain Res Mol Brain Res 1994;23: 163-78.
39. Pazos A, Cortes R, Palacios JM. Quantitative autoradiographic mapping of serotonin receptors in the rat brain. II. Serotonin-2 receptors. Brain Res 1985;346:231-49.
40. 2A serotonin receptors in the primate cerebral cortex: possible site of action of hallucinogenic and antipsychotic drugs in pyramidal cell apical dendrites. Proc Natl Acad Sci U S A 1998;95:735-40.
41. 2A receptors. Soc Neurosci Abstr 1997;23:385.
42. Cowburn D. Peptide recognition by PTB and PDZ domains. Curr Opin Struct Biol 1997;7:835-8.
43. Ranganathan R, Ross EM. PDZ domain proteins: scaffolds for signaling complexes. Curr Biol 1997;7:R770-R3.
44. 2C): where structure meets function. Pharmacol Ther 1998;79:231-57.
45. Roth BL, Ciaranello RD. Chronic mianserin treatment decreases 5-HT2 receptor binding without altering 5-HT2 receptor mRNA levels. Eur J Pharmacol 1991;207:169-72.
46. 2A receptors: a review of in vivo studies. Behav Brain Res 1996;73:177-81.
47. Burnet PW, Michelson D, Smith MA, Gold PW, Sternberg EM. The effect of chronic imipramine administration on the densities of 5-HT1A and 5-HT2 receptors and the abundances of 5-HT receptor and transporter mRNA in the cortex, hippocampus and dorsal raphe of three strains of rat. Brain Res 1994;638:311-24.
48. Burnet PW, Chen CP, McGowan S, Franklin M, Harrison PJ. The effects of clozapine and haloperidol on serotonin-1A, -2A and -2C receptor gene expression and serotonin metabolism in the rat forebrain. Neuroscience 1996;73:531-40.
49. 2C receptors stably expressed in the human neuroblastoma cell line SH-SY5Y. J Neurochem 1997;69:1031-8.
50. 2A receptors in vitro and in vivo. Ann N Y Acad Sci 1998;861:121-7.
51. Willins DL, Berry SA, Alsayegh L, Backstrom JR, Sanders-Bush E, Friedman L, et al. Clozapine and other 5-hydroxytrypatmine-2A receptor antagonists alter the subcellular distribution of 5-hydroxytryptamine-2A receptors in vitro and in vivo. Neuroscience 1999;91:599-606.
52. Morilak DA, Garlow SJ, Ciaranello RD. Immunocytochemical localization and description of neurons expressing serotonin2 receptors in the rat brain. Neuroscience 1993;54:701-17.
53. Mengood G, Pompeiano M, Martinez-Mir I, Palacios JM. Localization of the mRNA for the 5-HT2 receptor by in situ hybridization histochemistry. Brain Res 1990;524:139-43.
54. Seeman PCR, Van Tol HHM. Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors. Neuropsychopharmacol 1997;16:93-135.
55. Seeman P, Van Tol HH. Dopamine receptor pharmacology. Trends Pharmacol Sci 1994;15:264-70.
56. Costa T, Herz A. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc Natl Acad Sci U S A 1989;86:7321-5.
57. Scheer AFF, Costa T, De Benedetti PG, Cotecchia S. Constitutively active mutants of the alpha 1B-adrenergic receptor: role of highly conserved polar amino acids in receptor activation. EMBO J 1996;15:3566-78.
58. Samama PPG, Costa T, Cotecchia S, Lefkowitz RJ. Negative antagonists promote an inactive conformation of the β2-adrenergic receptor. Mol Pharmacol 1994;45:390-4.
59. Attramadal H, Arriza JL, Aoki C, Dawson TM, Codina J, Kwatra MM, et al. β-Arrestin 2, a novel member of the arrestin/β-arrestin gene family. J Biol Chem 1992;267:17882-90.
60. Allen PB, Ouimet CC, Greengard P. Spinophilin, a novel protein phosphatase 1 binding protein localized to dendritic spines. Proc Natl Acad Sci U S A 1997;94:9956-61.
61. Gelber EI, Kroeze WK, Willins DL, Gray JA, Sinar CA, Hyde EG, et al. Structure and function of the third intracellular loop of the 5-hydroxytryptamine2A receptor: the third intracellular loop is α-helical and binds purified arrestins. J Neurochem 1999;72: 2206-14.