The selective 5-HT(1B) receptor inverse agonist 1-methyl-5-[[2'-methyl- 4'(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7- 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

Volumn 41, Issue 8, 1998, Pages 1218-1235

  Gaster, Laramie M ^a,b   Blaney, Frank E ^a,b   Davies, Susannah ^a,b   Duckworth, D Malcolm ^a,b   Ham, Peter ^a,b   Jenkins, Sarah ^a,b   Jennings, Andrew J ^a,b   Joiner, Graham F ^a,b   King, Frank D ^a,b   Mulholland, Keith R ^a,b   Wyman, Paul A ^a,b   Hagan, Jim J ^a,b   Hatcher, Jon ^a,b   Jones, Brian J ^a,b   Middlemiss, Derek N ^a,b   Price, Gary W ^a,b   Riley, Graham ^a,b   Roberts, Claire ^a,b   Routledge, Carol ^a,b   Selkirk, Julie ^a,b   Slade, Paula D ^a,b   more..

^a GLAXOSMITHKLINE   (United Kingdom)

^b Department of Medicinal Chemistry ^*

Author keywords

[No Author keywords available]

Indexed keywords

2,3,6,7 TETRAHYDRO 1' METHYL 5 [[2' METHYL 4' (5 METHYL 1,2,4 OXADIAZOL 3 YL) 4 BIPHENYLYL]CARBONYL]SPIRO[FURO[2,3 F]INDOLE 3,4' PIPERIDINE]; KETANSERIN; METITEPINE; N [4 METHOXY 3 (4 METHYL 1 PIPERAZINYL)PHENYL] 2' METHYL 4' (5 METHYL 1,2,4 OXADIAZOL 3 YL)[1,1' BIPHENYL] 4 CARBOXAMIDE; RITANSERIN; SEROTONIN 1B AGONIST; SEROTONIN 1D RECEPTOR; UNCLASSIFIED DRUG; 3 (2 DIMETHYLAMINOETHYL) 4 CHLORO 5 PROPOXYINDOLE; ASPARTIC ACID; AUTORECEPTOR; HTR1B PROTEIN, HUMAN; INDOLE DERIVATIVE; OXADIAZOLE DERIVATIVE; PIPERAZINE DERIVATIVE; PIPERIDONE DERIVATIVE; SB 22489G; SEROTONIN 1B RECEPTOR; SEROTONIN AGONIST; SEROTONIN ANTAGONIST; SEROTONIN RECEPTOR; SPIRO COMPOUND;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG DISCRIMINATION; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; GUINEA PIG; HUMAN; MALE; NONHUMAN; ORAL DRUG ADMINISTRATION; SEROTONINERGIC SYSTEM; STRUCTURE ACTIVITY RELATION; THERMOREGULATION; ANIMAL; CHEMICAL STRUCTURE; CHEMICALLY INDUCED DISORDER; CHEMISTRY; CHO CELL; COMPARATIVE STUDY; DRUG ANTAGONISM; DRUG EFFECT; FRONTAL LOBE; HAMSTER; HYPOTHERMIA; IN VITRO STUDY; METABOLISM; RADIOASSAY; RAT; SWINE; SYNTHESIS;

ANIMALS; ASPARTIC ACID; AUTORECEPTORS; CHO CELLS; CRICETINAE; FRONTAL LOBE; GUINEA PIGS; HUMANS; HYPOTHERMIA; INDOLES; MALE; MODELS, MOLECULAR; OXADIAZOLES; PIPERAZINES; PIPERIDONES; RADIOLIGAND ASSAY; RATS; RECEPTOR, SEROTONIN, 5-HT1B; RECEPTOR, SEROTONIN, 5-HT1D; RECEPTORS, SEROTONIN; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; SPIRO COMPOUNDS; STRUCTURE-ACTIVITY RELATIONSHIP; SWINE;

EID: 14444273648     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm970457s     Document Type: Article

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