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

被引:10
作者
BLUM, E [1 ]
BUCHHEIT, KH [1 ]
BUESCHER, HH [1 ]
GAMSE, R [1 ]
KLOEPPNER, E [1 ]
MEIGEL, H [1 ]
PAPAGEORGIOU, C [1 ]
WAELCHLI, R [1 ]
REVESZ, L [1 ]
机构
[1] SANDOZ PHARM AG,PRECLIN RES,CH-4002 BASEL,SWITZERLAND
关键词
D O I
10.1016/S0960-894X(00)80170-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A novel highly potent 5-HT3 antagonist and Tropisetron analogue (1) is described with an increased efficacy to inhibit cisplatin induced emesis in ferrets. Four novel structural classes of gastroprokinetic benzamide bioisosteres (8-11) are presented. 5-HT derivatives 12-14 are described as ligands of the recently discovered 5-HT4 receptor.
引用
收藏
页码:461 / 466
页数:6
相关论文
共 18 条
[1]   PROPOSALS FOR THE CLASSIFICATION AND NOMENCLATURE OF FUNCTIONAL RECEPTORS FOR 5-HYDROXYTRYPTAMINE [J].
BRADLEY, PB ;
ENGEL, G ;
FENIUK, W ;
FOZARD, JR ;
HUMPHREY, PPA ;
MIDDLEMISS, DN ;
MYLECHARANE, EJ ;
RICHARDSON, BP ;
SAXENA, PR .
NEUROPHARMACOLOGY, 1986, 25 (06) :563-576
[2]   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
[3]  
BUCHHEIT KH, 1985, N-S ARCH PHARMACOL, V329, P26
[4]  
BUTLER A, 1988, EUR J PHARMACOL, V159, P113
[5]   THE 5-HT4 RECEPTOR - NAUGHTY, BUT NICE [J].
CLARKE, DE ;
CRAIG, DA ;
FOZARD, JR .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1989, 10 (10) :385-386
[6]   PERISTALSIS EVOKED BY 5-HT AND RENZAPRIDE - EVIDENCE FOR PUTATIVE 5-HT4 RECEPTOR ACTIVATION [J].
CRAIG, DA ;
CLARKE, DE .
BRITISH JOURNAL OF PHARMACOLOGY, 1991, 102 (03) :563-564
[7]  
CRAIG DA, 1990, J PHARMACOL EXP THER, V252, P1378
[8]   THE GASTROINTESTINAL PROKINETIC BENZAMIDE DERIVATIVES ARE AGONISTS AT THE NON-CLASSICAL 5-HT RECEPTOR (5-HT4) POSITIVELY COUPLED TO ADENYLATE-CYCLASE IN NEURONS [J].
DUMUIS, A ;
SEBBEN, M ;
BOCKAERT, J .
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1989, 340 (04) :403-410
[9]   IDENTIFICATION OF PUTATIVE 5-HT4-RECEPTORS IN GUINEA-PIG ASCENDING COLON [J].
ELSWOOD, CJ ;
BUNCE, KT ;
HUMPHREY, PPA .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 196 (02) :149-155
[10]  
FAKE C S, 1987, British Journal of Pharmacology, V91, p335P