KETONES RELATED TO THE BENZOATE 5-HT4 RECEPTOR ANTAGONIST RS-23597 ARE HIGH-AFFINITY PARTIAL AGONISTS

被引：20

作者：

CLARK, RD

JAHANGIR, A

LANGSTON, JA

WEINHARDT, KK

MILLER, AB

LEUNG, E

EGLEN, RM

机构：

[1] SYNTEX INC,INST ANALYT RES,PALO ALTO,CA 94304

[2] SYNTEX INC,INST PHARMACOL,PALO ALTO,CA 94304

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(01)80413-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The ketone analogue 5 of the 5-HT4 receptor antagonist RS-23597 (1) was found to be a 5HT(4) receptor partial agonist. Structure-activity relationships developed for compound 5 led to the synthesis of 4-piperidinyl derivatives (15-18, 20) that were found to be partial agonists with increased affinity.

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页码：2477 / 2480

页数：4

相关论文

共 16 条

[1]

BAXTER GS, 1991, N-S ARCH PHARMACOL, V343, P439

[2]

BAXTER GS, 1993, BIOMED CHEM LETT, V3, P461

[3] DESIGN AND SYNTHESIS OF NOVEL LIGANDS FOR THE 5-HT(3) AND THE 5-HT(4) RECEPTOR [J].

BLUM, E ;

BUCHHEIT, KH ;

BUESCHER, HH ;

GAMSE, R ;

KLOEPPNER, E ;

MEIGEL, H ;

PAPAGEORGIOU, C ;

WAELCHLI, R ;

REVESZ, L .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1992, 2 (05) :461-466

[4] SDZ-205-557, A SELECTIVE ANTAGONIST AT 5-HT4 RECEPTORS IN THE ISOLATED GUINEA-PIG ILEUM [J].

BUCHHEIT, KH ;

GAMSE, R ;

PFANNKUCHE, HJ .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 200 (2-3) :373-374

[5] 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

[6] N-(QUINUCLIDIN-3-YL)-1,8-NAPHTHALIMIDES WITH 5-HT(3) RECEPTOR ANTAGONIST AND 5-HT(4) RECEPTOR AGONIST PROPERTIES [J].

CLARK, RD ;

WEINHARDT, KK ;

BERGER, J ;

LEE, CH ;

LEUNG, E ;

WONG, EHF ;

SMITH, WL ;

EGLEN, RM .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (06) :1375-1378

[7] RS-23597-190 - A POTENT AND SELECTIVE 5-HT4 RECEPTOR ANTAGONIST [J].

EGLEN, RM ;

BLEY, K ;

BONHAUS, DW ;

CLARK, RD ;

HEGDE, SS ;

JOHNSON, LG ;

LEUNG, E ;

WONG, EHF .

BRITISH JOURNAL OF PHARMACOLOGY, 1993, 110 (01) :119-126

[8] 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

[9]

FLYNN DL, 1992, J MED CHEM, V35, P1489

[10]

FORD APD, 1993, MED RES REV, P633