Substituted pyrazoles as novel selective ligands for the human dopamine D4 receptor

被引：20

作者：

Bourrain, S ^{[1
]}

Collins, I ^{[1
]}

Neduvelil, JG ^{[1
]}

Rowley, M ^{[1
]}

Leeson, PD ^{[1
]}

Patel, S ^{[1
]}

Emms, F ^{[1
]}

Marwood, R ^{[1
]}

Chapman, KL ^{[1
]}

Fletcher, AE ^{[1
]}

Showell, GA ^{[1
]}

机构：

[1] Merck Sharp & Dohme Res Labs, Neurosci Res Ctr, Harlow CM20 2QR, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1998年 / 6卷 / 10期

关键词：

dopamine; hD(4); affinity; selectivity; pyrazole;

D O I：

10.1016/S0968-0896(98)00134-5

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Two novel series of 3-(heterocyclylmethyl)pyrazoles have been synthesised and evaluated as ligands for the human dopamine D-4 receptor. Compounds in series I (exemplified by 8k) have a phenyl ring joined to the 4-position of the pyrazole while those in series II (exemplified by 15j) have a 5-phenyl ring linked by a saturated chain to the 4-position of the pyrazole. Both series supplied compounds with excellent affinity for the human D-4 and good selectivity over other dopamine receptors. Excellent selectivity over calcium, sodium, and potassium ion channels was also achieved. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1731 / 1743

页数：13

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