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.

引用

页码：715 / 719

页数：5

共 24 条

[1] EFFECTS OF THE 5-HT3 RECEPTOR ANTAGONIST, GR38032F, ON RAISED DOPAMINERGIC ACTIVITY IN THE MESOLIMBIC SYSTEM OF THE RAT AND MARMOSET BRAIN
COSTALL, B
DOMENEY, AM
NAYLOR, RJ
TYERS, MB
[J]. BRITISH JOURNAL OF PHARMACOLOGY, 1987, 92 (04) : 881 - 894
[2] THE GASTROINTESTINAL PROKINETIC BENZAMIDE DERIVATIVES ARE AGONISTS AT THE NON-CLASSICAL 5-HT RECEPTOR (5-HT4) POSITIVELY COUPLED TO ADENYLATE-CYCLASE IN NEURONS
DUMUIS, A
SEBBEN, M
BOCKAERT, J
[J]. NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1989, 340 (04) : 403 - 410
[3] MOLECULAR MODELING OF 5-HT3 RECEPTOR LIGANDS
EVANS, SM
GALDES, A
GALL, M
[J]. PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 1991, 40 (04) : 1033 - 1040
[4] Gray JA., 1982, NEUROPSYCHOLOGY ANXI
[5] ANTIMALARIALS - SYNTHESIS AND ANTIMALARIAL ACTIVITY OF 1-(4-METHOXYCINNAMOYL)-4-(5-PHENYL-4-OXO-2-OXAZOLIN-2-YL)PIPERAZINE AND DERIVATIVES
HERRIN, TR
PAUVLIK, JM
SCHUBER, EV
GEISZLER, AO
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1975, 18 (12) : 1216 - 1223
[6] MOLECULAR PHARMACOLOGY OF 5-HT1 AND 5-HT2 RECOGNITION SITES IN RAT AND PIG BRAIN MEMBRANES - RADIOLIGAND BINDING-STUDIES WITH [H-3] 5-HT, [H-3] 8-OH-DPAT, (-) [I-125] IODOCYANOPINDOLOL, [H-3] MESULERGINE AND [H-3] KETANSERIN
HOYER, D
ENGEL, G
KALKMAN, HO
[J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1985, 118 (1-2) : 13 - 23
[7] 5-HT AND ANXIETY - PROMISES AND PITFALLS
JOHNSTON, AL
FILE, SE
[J]. PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 1986, 24 (05) : 1467 - 1470
[8] THE POTENTIAL ANXIOLYTIC ACTIVITY OF GR38032F, A 5-HT3-RECEPTOR ANTAGONIST
JONES, BJ
COSTALL, B
DOMENEY, AM
KELLY, ME
NAYLOR, RJ
OAKLEY, NR
TYERS, MB
[J]. BRITISH JOURNAL OF PHARMACOLOGY, 1988, 93 (04) : 985 - 993
[9] MOLECULAR-CLONING OF A SEROTONIN RECEPTOR FROM HUMAN BRAIN (5HT1E) - A 5TH 5HT1-LIKE SUBTYPE
MCALLISTER, G
CHARLESWORTH, A
SNODIN, C
BEER, MS
NOBLE, AJ
MIDDLEMISS, DN
IVERSEN, LL
WHITING, P
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (12) : 5517 - 5521
[10] MELTZER HY, 1991, 5TH WORLD C BIOL PSY

← 1 2 3 →