Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT(2C) receptor inverse agonist but fails to induce 5-HT(2C) receptor down- regulation

Psychopharmacology

Volumn 136, Issue 2, 1998, Pages 99-104

  Pälvimäki, Esa Pekka ^a   Majasuo, Hannu ^a   Kuoppamäki, Mikko ^a   Männistö, Pekka T ^b   Syvälahti, Erkka ^a   Hietala, Jarmo ^a  

^a UNIVERSITY OF TURKU   (Finland)

^b UNIVERSITY OF EASTERN FINLAND   (Finland)

Author keywords

5HT(2A); 5HT(2C); Anxiolytic drug; Deramciclane; Inverse agonist; Receptor regulation; Serotonin receptor

Indexed keywords

ANXIOLYTIC AGENT; DERAMCICLANE FUMARATE; SEROTONIN 2C AGONIST; SEROTONIN 2C RECEPTOR;

ANIMAL EXPERIMENT; ANXIETY NEUROSIS; ARTICLE; DOWN REGULATION; DRUG RECEPTOR BINDING; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY;

ANIMALS; ANTI-ANXIETY AGENTS; BORNANES; BRAIN; CLOZAPINE; INOSITOL PHOSPHATES; MALE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTOR, SEROTONIN, 5-HT2C; RECEPTORS, SEROTONIN; SEROTONIN ANTAGONISTS;

EID: 0031884405     PISSN: 00333158     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002130050544     Document Type: Article

References (31)

1. Baldessarini RJ, Centorrino F, Flood JG, Volpicelli SA, Huston-Lyons D, Cohen BM (1993) Tissue concentrations of clozapine and its metabolites in the rat. Neuropsychopharmacology 9:117-124
2. 1C receptor density and mRNA levels in choroid plexus epithelial cells after treatment with mianserin and (-)-1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane. Mol Pharmacol 44: 725-730
3. 1C receptors. Naunyn-Schmiedeberg's Arch Pharmacol 348:221-224
4. 2C receptor-mediated phosphoinositide turnover and the stimulus effects of m-chlorophenylpiperazine. Psychopharmacology 122: 237-243
5. Gacsályi I, Gyertyán I, Petöcz L, Budai Z (1988) Psychopharmacology of a new anxiolytic agent EGYP-3886. Pharmacol Res Commun 20:115-117
6. 2 receptors. Pharm Pharmacol Lett 6:82-85
7. Gardner CR (1986) Recent developments in 5-HT-related pharmacology of animal models of anxiety. Pharmacol Biochem Behav 24:1479-1485
8. 2C receptors but not by sympathomimetic effects. Neuropharmacology 33:457-465
9. Gleeson S, Ahlers ST, Mansbach RS, Foust JM, Barrett JE (1989) Behavioural studies with anxiolytic drugs. VI: Effects on punished responding of drugs interacting with serotonin receptor subtypes. J Pharmacol Exp Ther 250:809-817
10. Griebel G (1995) 5-Hydroxytryptamine-interacting drugs in animal models of anxiety disorders: more than 30 years of research. Pharmacol Ther 65:319-395
11. Handley SL, McBlane JW (1993) 5-HT drugs in animal models of anxiety. Psychopharmacology 112:13-20
12. Hietala J, Koulu M, Kuoppamäki M, Lappalainen J, Syvälahti E (1992) Chronic clozapine treatment down-regulates serotonin 5-HT-1c receptors in rat brain. Prog Neuropsychopharmacol Biol Psychiatry 16:727-732
13. Kahn RS, Van Praag HM, Wetzler S, Asnis GM, Barr G (1988) Serotonin and anxiety revisited. Biol Psychiatry 23:189-208
14. 1C receptor antagonists. Eur J Pharmacol 164: 445-454
15. 1C receptor antagonists have anxiolytic-like actions in the rat social interaction test. Psychopharmacology 107:379-384
16. 1C receptors and their therapeutic relevance. Curr Opin Invest Drugs 2:317-362
17. 1C receptor-mediated phosphoinositide hydrolysis in the rat choroid plexus after chronic treatment with clozapine. Eur J Pharmacol 255:91-97
18. 2C receptors in the rat choroid plexus. Neuropsychopharmacology 15:143-151
19. Labrecque J, Fargin A, Bouvier M, Chidiac P, Dennis M (1995) Serotonergic antagonists differentially inhibit spontaneous activity and decrease ligand binding capacity of the rat 5-hydroxytryptamine type 2C receptor in Sf9 cells. Mol Pharmacol 48:150-159
20. Milligan G, Bond RA, Lee M (1995) Inverse agonism: pharmacological curiosity or potential therapeutic strategy? Trends Pharmacol Sci 16:10-13
21. 2C receptor. Psychopharmacology 126:234-240
22. Peroutka SJ, Snyder SH (1980) Long-term antidepressant treatment decreases spiroperidol-labeled serotonin receptor binding. Science 210:88-90
23. 2 receptors in rat cortex. Studies with a putative selective agonist and an antagonist. Biochem Pharmacol 42:1099-1105
24. 1C/2 receptor agonists and antagonists. Eur J Pharmacol [Mol Pharmacol Sect] 244:1-5
25. 2 receptors in mouse brain. Mol Pharmacol 43:84-89
26. 2C receptor levels. Eur J Pharmacol 262:125-131
27. 1C serotonin receptor levels. Methodology and mechanisms. Neuropsychopharmacology 3:427-433
28. Sanders-Bush E, Breeding M (1988) Putative selective 5-HT-2 antagonists block serotonin 5-HT-1c receptors in the choroid plexus. J Pharmacol Exp Ther 247:169-173
29. Sanders-Bush E, Breeding M (1990) Serotonin1creceptor reserve in choroid plexus masks receptor subsensitivity. J Pharmacol Exp Ther 252:984-988
30. Shenker A, Kosugi S, Meredino JJ Jr, Minegishi T, Cutler GB Jr (1993) A constitutively activating mutation of the luteinizing hormone receptor in familial male precocious puberty. Nature 365:652-654
31. Westphal RS, Backstrom JR, Sanders-Bush E (1995) Increased basal phosphorylation of the constitutively active serotonin 2C receptor accompanies agonist-mediated desensitization. Mol Pharmacol 48:200-205