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Titolo:
IN-VIVO PROPERTIES OF SB 200646A, A 5-HT2C 2B RECEPTOR ANTAGONIST/
Autore:
KENNETT GA; WOOD MD; GLEN A; GREWAL S; FORBES I; GADRE A; BLACKBURN TP;
Indirizzi:
SMITHKLINE BEECHAM,DEPT PSYCHIAT,COLDHARBOUR RD HARLOW CM19 5AD ESSEXENGLAND SMITHKLINE BEECHAM,DEPT MED CHEM HARLOW CM19 5AD ESSEX ENGLAND
Titolo Testata:
British Journal of Pharmacology
fascicolo: 3, volume: 111, anno: 1994,
pagine: 797 - 802
SICI:
0007-1188(1994)111:3<797:IPOS2A>2.0.ZU;2-W
Fonte:
ISI
Lingua:
ENG
Soggetto:
5-HT1C RECEPTOR; M-CHLOROPHENYLPIPERAZINE; SEROTONIN-1 RECEPTORS; DEPRESSIVE-ILLNESS; ANXIETY DISORDERS; CHOROID-PLEXUS; ANIMAL-MODELS; MESSENGER-RNA; RAT-BRAIN; MCPP;
Keywords:
5-HT2C RECEPTORS; 5-HT2A RECEPTORS; 5-HT2B RECEPTORS; 5-HT; ANXIETY; SB 200646A;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
46
Recensione:
Indirizzi per estratti:
Citazione:
G.A. Kennett et al., "IN-VIVO PROPERTIES OF SB 200646A, A 5-HT2C 2B RECEPTOR ANTAGONIST/", British Journal of Pharmacology, 111(3), 1994, pp. 797-802

Abstract

1 SB 200646A, N-(1-methyl-5-indolyl)-N-(3-pyridyl) urea hydro chloride, the first reported selective 5-HT2C/2B over 5-HT2A receptor antagonist, (pK(l) rat 5-HT2C receptor 6.9, pA(2) rat 5-HT2B receptor 7.5, pK(l) rat 5-HT2A receptor 5.2) dose-dependently blocked a putative rat model of 5-HT2C receptor activation; 1-(3-chlorophenyl)piperazine (mCPP, 5 mg kg(-1), i.p. 20 min pretest)-induced hypolocomotion (estimated ID50 19.2 mg kg(-1), p.o.). 2 SB 200646A also blocked another putativein vivo model of 5-HT2C receptor function; mCPP (5 mg kg(-1), i.p. 20min pretest)-induced hypophagia in 23 h food-deprived rats (estimatedID50 18.3 mg kg(-1), p.o.). 3 SB 200646A did not antagonize 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI)-induced head shakes in ratsat doses up to 200 mg kg(-1), p.o., an effect thought to be mediated by 5-HT2A receptors for which SB 200646A has its next highest affinity(50 fold less) after the 5-HT2C and 5-HT2B sites. 4 SB 200646A (20, 40 mg kg(-1), p.o., 1h pretest) also reversed mCPP (0.5 mg kg(-1), i.p., 30 min pretest)-induced anxiety in the social interaction test, under low light familiar conditions. 5 When given alone, under high light unfamiliar conditions, SB 200646A (2-40 mg kg(-1), p.o.) increased active social interaction without affecting locomotor activity in the ratsocial interaction test. This is consistent with an anxiolytic actionof SB 200646A. 6 These results indicate that SB 200646A has in vivo efficacy and that 5-HT2C or 5-HT2B receptors are indeed likely to mediate mCPP-induced hypolocomotion, hypophagia and anxiogenesis. They alsosuggest that 5-HT2C/2B receptor blockade induces anxiolysis.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/03/20 alle ore 09:34:31