Studies towards the next generation of antidepressants. Part 1: Indolylcyclohexylamines as potent serotonin reuptake inhibitors

被引:35
作者
Meagher, KL [1 ]
Mewshaw, RE [1 ]
Evrard, DA [1 ]
Zhou, P [1 ]
Smith, DL [1 ]
Scerni, R [1 ]
Spangler, T [1 ]
Abulhawa, S [1 ]
Shi, XJ [1 ]
Schechter, LE [1 ]
Andree, TH [1 ]
机构
[1] Wyeth Ayerst Res Labs, Global Chem Sci & Neurosci Dept, Princeton, NJ 08543 USA
关键词
D O I
10.1016/S0960-894X(01)00334-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of indolylcyclohexylamines possessing potent and selective serotonin reuptake inhibition is reported. The most interesting compounds proved to have subnanomolar 5-HT transporter activity, and exhibited moderate 5-HT1A affinity. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1885 / 1888
页数:4
相关论文
共 20 条
[1]   CONTEMPORARY MANAGEMENT OF DEPRESSION [J].
ANDREWS, JM ;
NEMEROFF, CB .
AMERICAN JOURNAL OF MEDICINE, 1994, 97 :S24-S32
[2]   Acceleration of the effect of selected antidepressant drugs in major depression by 5-HT1A antagonists [J].
Artigas, F ;
Romero, L ;
deMontigny, C ;
Blier, P .
TRENDS IN NEUROSCIENCES, 1996, 19 (09) :378-383
[3]  
ARTIGAS F, 1994, ARCH GEN PSYCHIAT, V51, P248
[4]   ADVERSE-EFFECTS OF ANTI-DEPRESSANT DRUGS .1. MONOAMINE-OXIDASE INHIBITORS AND TRICYCLICS [J].
BLACKWELL, B .
DRUGS, 1981, 21 (03) :201-219
[5]  
Blier P, 1998, J CLIN PSYCHIAT, V59, P16
[6]   EFFECTIVENESS OF PINDOLOL WITH SELECTED ANTIDEPRESSANT DRUGS IN THE TREATMENT OF MAJOR DEPRESSION [J].
BLIER, P ;
BERGERON, R .
JOURNAL OF CLINICAL PSYCHOPHARMACOLOGY, 1995, 15 (03) :217-222
[7]   [H-3] PAROXETINE BINDING IN RAT FRONTAL-CORTEX STRONGLY CORRELATES WITH [H-3] 5-HT UPTAKE - EFFECT OF ADMINISTRATION OF VARIOUS ANTIDEPRESSANT TREATMENTS [J].
CHEETHAM, SC ;
VIGGERS, JA ;
SLATER, NA ;
HEAL, DJ ;
BUCKETT, WR .
NEUROPHARMACOLOGY, 1993, 32 (08) :737-743
[8]  
CIPOLLINA JA, 1995, Patent No. 5468767
[9]   Characterization of 5-HT1A receptor functional coupling in cells expressing the human 5-HT1A receptor as assessed with the cytosensor microphysiometer [J].
Dunlop, J ;
Zhang, YX ;
Smith, DL ;
Schechter, LE .
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS, 1998, 40 (01) :47-55
[10]  
GEORGIAN V, 1962, J ORG CHEM, P4571