RS-100235 - A HIGH-AFFINITY 5-HT4 RECEPTOR ANTAGONIST

被引:17
作者
CLARK, RD [1 ]
JAHANGIR, A [1 ]
FLIPPIN, LA [1 ]
LANGSTON, JA [1 ]
LEUNG, E [1 ]
BONHAUS, DW [1 ]
WONG, EHF [1 ]
JOHNSON, LG [1 ]
EGLEN, RM [1 ]
机构
[1] SYNTEX INC,INST PHARMACOL,PALO ALTO,CA 94304
关键词
D O I
10.1016/0960-894X(95)00358-Z
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The 1,4-benzodioxanyl ketone 14 (RS-100235) was found to be high affinity 5-HT4 antagonist with potent in vivo activity and a sustained duration of action in the anesthetized pig.
引用
收藏
页码:2119 / 2122
页数:4
相关论文
共 11 条
[1]  
BAXTER GS, 1991, N-S ARCH PHARMACOL, V343, P439
[2]   SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF 2-BENZYLOXY SUBSTITUTED ARYL KETONES AS 5-HT4 RECEPTOR ANTAGONISTS [J].
CLARK, RD ;
JAHANGIR, A ;
LANGSTON, JA ;
WEINHARDT, KK ;
MILLER, AB ;
LEUNG, E ;
BONHAUS, DW ;
WONG, EHF ;
EGLEN, RM .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (20) :2481-2484
[3]   THE ACTION OF SDZ 205,557 AT 5-HYDROXYTRYPTAMINE (5-HT3 AND 5-HT4) RECEPTORS [J].
EGLEN, RM ;
ALVAREZ, R ;
JOHNSON, LG ;
LEUNG, E ;
WONG, EHF .
BRITISH JOURNAL OF PHARMACOLOGY, 1993, 108 (02) :376-382
[4]   THE 5-HT(4)- RECEPTOR [J].
FORD, APDW ;
CLARKE, DE .
MEDICINAL RESEARCH REVIEWS, 1993, 13 (06) :633-662
[5]   (1-BUTYL-4-PIPERIDINYL)METHYL 8-AMINO-7-CHLORO-1,4-BENZODIOXANE-5-CARBOXYLATE HYDROCHLORIDE - A HIGHLY POTENT AND SELECTIVE 5-HT4 RECEPTOR ANTAGONIST DERIVED FROM METOCLOPRAMIDE [J].
GASTER, LM ;
JENNINGS, AJ ;
JOINER, GF ;
KING, FD ;
MULHOLLAND, KR ;
RAHMAN, SK ;
STARR, S ;
WYMAN, PA ;
WARDLE, KA ;
ELLIS, ES ;
SANGER, GJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (25) :4121-4123
[6]   DEVELOPMENT OF A RADIOLIGAND BINDING ASSAY FOR 5-HT(4)-RECEPTORS IN GUINEA-PIG AND RAT-BRAIN [J].
GROSSMAN, CJ ;
KILPATRICK, GJ ;
BUNCE, KT .
BRITISH JOURNAL OF PHARMACOLOGY, 1993, 109 (03) :618-624
[7]  
GROSSMAN CJ, 1994, BRIT J PHARMACOL, V111, P332
[8]  
HEDE SS, 1994, J PHARMACOL EXP THER, V271, P741
[9]   DERIVATIVES OF BENZO-1-4-DIOXAN .1. SOME HALOGENATED BENZO-1-4-DIOXANS AND AMINO-DERIVATIVES AND NITRO-DERIVATIVES THEREOF [J].
HEERTJES, PM ;
KNAPE, AA ;
TALSMA, H ;
ANDRIESSE, P .
JOURNAL OF THE CHEMICAL SOCIETY, 1954, (JAN) :18-22
[10]   MEDIATION OF 5-HYDROXYTRYPTAMINE-INDUCED TACHYCARDIA IN THE PIG BY THE PUTATIVE 5-HT4-RECEPTOR [J].
VILLALON, CM ;
DENBOER, MO ;
HEILIGERS, JPC ;
SAXENA, PR .
BRITISH JOURNAL OF PHARMACOLOGY, 1990, 100 (04) :665-667