SYNTHESIS AND EVALUATION OF NEW 2-PIPERAZINYLBENZOTHIAZOLES WITH HIGH 5-HT1A AND 5-HT3 AFFINITIES

被引：30
作者：
DIOUF, O
DEPREUX, P
LESIEUR, D
POUPAERT, JH
CAIGNARD, DH
机构：
[1] UNIV CATHOLIQUE LOUVAIN,ECOLE PHARM,B-1200 BRUSSELS,BELGIUM
[2] FAC PHARM LILLE,CHIM THERAPEUT LAB,F-59006 LILLE,FRANCE
[3] ADIR & CIE,F-92415 COURBEVOIE,FRANCE
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 30卷 / 09期
关键词：
BENZOTHIAZOLE; BENZOTHIAZOLIN-2-ONE; SEROTONIN; 5-HT1A RECEPTOR; 5-HT3; RECEPTOR; PSYCHOTROPIC DISEASE;
D O I：
10.1016/0223-5234(96)88289-4
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Original 2-piperazinylbenzothiazole derivatives were synthesized and studied as mixed ligands for serotoninergic 5-HT1A and 5-HT3 receptors. The studied compounds exhibited significant affinities for these two serotoninergic receptor subtypes. The pharmacological profile of these ligands was agonist for 5-HT1A receptors and antagonist for 5-HT3 receptor subsites. Compounds with such a pharmacological profile are of clinical relevance in the treatment of psychotropic diseases (eg, anxiety, depression and schizophrenia). The present paper reports the chemistry and the in vitro pharmacological evaluation of these ligands.
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页码：715 / 719
页数：5
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