N-[3-(1H-imidazol-4-ylmethyl)phenyl]-ethanesulfonamide (ABT-866, 1),1 a novel α1-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine

被引：9

作者：

Altenbach, RJ ^{[1
]}

Khilevich, A ^{[1
]}

Meyer, MD ^{[1
]}

Buckner, SA ^{[1
]}

Milicic, I ^{[1
]}

Daza, AV ^{[1
]}

Brune, ME ^{[1
]}

O'Neill, AB ^{[1
]}

Gauvin, DM ^{[1
]}

Cain, JC ^{[1
]}

Nakane, M ^{[1
]}

Holladay, MW ^{[1
]}

Williams, M ^{[1
]}

Brioni, JD ^{[1
]}

Sullivan, JP ^{[1
]}

机构：

[1] Abbott Labs, Global Pharmaceut Res & Dev, Neurosci Res, Abbott Pk, IL 60064 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 20期

关键词：

D O I：

10.1021/jm025550h

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1) is a novel alpha(1) agent having the unique profile of alpha(1A) (rabbit urethra, EC50 = 0.60 muM) agonism with alpha(1B) (rat spleen, pA(2) = 5.4) and alpha(1D) (rat aorta, pA(2) = 6.2) antagonism. An in vivo dog model showed I to be more selective for the urethra over the vasculature than A-61603 (2), ST-1059 (3, the active metabolite of midodrine), and phenylpropanolamine (4).

引用

页码：4395 / 4397

页数：3

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