Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H3 receptor agonist

被引：51

作者：

Kitbunnadaj, R

Zuiderveld, OP

Christophe, B

Hulscher, S

Menge, WMPB

Gelens, E

Snip, E

Bakker, RA

Celanire, S

Gillard, M

Talaga, P

Timmerman, H

Leurs, R ^{[1
]}

机构：

[1] Vrije Univ Amsterdam, LACDR, Div Med Chem, Fac Sci, Amsterdam, Netherlands

[2] Naresuan Univ, Dept Pharmaceut Chem & Pharmacognosy, Fac Pharmaceut Sci, Phitsanulok, Thailand

[3] UCB Pharma, B-1420 Braine lAlleud, Belgium

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 10期

关键词：

D O I：

10.1021/jm049932u

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this study, the piperidine ring of immepip and its analogues was replaced by a rigid heterocyclic pyridine ring. Many compounds in the series exhibit high affinity and agonist activity at the human histamine H-3 receptor. Particularly, the 4-pyridinyl analogue of immepip (1c, immethridine) is identified as a novel potent and highly selective histamine H3 receptor agonist (pK(i) = 9.07, pEC(50) = 9.74) with a 300-fold selectivity over the closely related H-4 receptor.

引用

页码：2414 / 2417

页数：4

共 33 条

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