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Titolo:
THE SELECTIVE 5-HT1B RECEPTOR INVERSE AGONIST TETRAHYDROSPIRO[FURO[2,3-F]INDOLE-3,4'-PIPERIDINE] (SB-224289) POTENTLY BLOCKS TERMINAL 5-HT AUTORECEPTOR FUNCTION BOTH IN-VITRO AND IN-VIVO
Autore:
GASTER LM; BLANEY FE; DAVIES S; DUCKWORTH DM; HAM P; JENKINS S; JENNINGS AJ; JOINER GF; KING FD; MULHOLLAND KR; WYMAN PA; HAGAN JJ; HATCHER J; JONES BJ; MIDDLEMISS DN; PRICE GW; RILEY G; ROBERTS C; ROUTLEDGE C; SELKIRK J; SLADE PD;
Indirizzi:
SMITHKLINE BEECHAM PHARMACEUT,DISCOVERY RES,DEPT MED CHEM,NEW FRONTIERS SCI PK N,3RD AVE HARLOW CM19 5AW ESSEX ENGLAND SMITHKLINE BEECHAM PHARMACEUT,DISCOVERY RES,DEPT NEUROSCI RES HARLOW CM19 5AW ESSEX ENGLAND
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 8, volume: 41, anno: 1998,
pagine: 1218 - 1235
SICI:
0022-2623(1998)41:8<1218:TS5RIA>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
RECOMBINANT HUMAN 5-HT1D-ALPHA; PIG FRONTAL-CORTEX; GUINEA-PIG; BRAIN CORTEX; 5-HT1D-BETA RECEPTORS; MEDIATING INHIBITION; ADRENERGIC-RECEPTOR; ANTAGONIST BINDING; GR127935 ACTS; SEROTONIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
57
Recensione:
Indirizzi per estratti:
Citazione:
L.M. Gaster et al., "THE SELECTIVE 5-HT1B RECEPTOR INVERSE AGONIST TETRAHYDROSPIRO[FURO[2,3-F]INDOLE-3,4'-PIPERIDINE] (SB-224289) POTENTLY BLOCKS TERMINAL 5-HT AUTORECEPTOR FUNCTION BOTH IN-VITRO AND IN-VIVO", Journal of medicinal chemistry, 41(8), 1998, pp. 1218-1235

Abstract

5-HT1 receptors are members of the G-protein-coupled receptor superfamily and are negatively Linked to adenylyl cyclase activity. The human5-HT1B and 5-HT1D receptors (previously known as 5-HT1D beta and 5-HT1D alpha, respectively), although encoded by two distinct genes, are structurally very similar. Pharmacologically, these two receptors have been differentiated using nonselective chemical tools such as ketanserin and ritanserin, but the absence of truly selective agents has meantthat the precise function of the 5-HT1B and 5-HT1D receptors has not been defined. In this paper we describe how, using computational chemistry models as a guide, the nonselective 5-HT1B/5-HT1D receptor antagonist 4 was structurally modified to produce the selective 5-HT1B receptor inverse agonist 5, tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289). This compound is a potent antagonist of terminal 5-HTautoreceptor function both in vitro and in vivo.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/08/20 alle ore 06:24:57