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Bioorg Med Chem Lett. 2006 Aug 1;16(15):4045-7. Epub 2006 May 24.

Design and synthesis of selective alpha1B adrenoceptor antagonists.

Author information

1
Pharmaceutical Research Laboratories, Toray Industries, Inc., 1111 Tebiro, Kamakura, Kanagawa 248-8555, Japan. ryoji_hayashi2@nts.toray.co.jp

Abstract

A series of novel indolylpiperidine derivatives were synthesized and assessed for their pharmacological profiles at alpha1 adrenoceptor subtypes by in vitro binding studies at rat alpha1A and alpha1B receptors. Compound 11 was a potent (Ki=0.63 nM) and selective (approximately 30-fold more selective for the alpha1B receptor than for the alpha1A receptor) alpha1B adrenoceptor antagonist.

PMID:
16723224
DOI:
10.1016/j.bmcl.2006.05.002
[Indexed for MEDLINE]

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