Design and synthesis of selective alpha1B adrenoceptor antagonists.
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.
Hayashi
Ryoji
R
Pharmaceutical Research Laboratories, Toray Industries, Inc., 1111 Tebiro, Kamakura, Kanagawa 248-8555, Japan. ryoji_hayashi2@nts.toray.co.jp
Ohmori
Eiji
E
Isogaya
Masafumi
M
Moriwaki
Mitsuhiro
M
Kumagai
Hiroki
H
D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis* / Q000737:chemistry; D015195:Drug Design; D018340:Receptors, Adrenergic, alpha-1
C547718:Adra1b protein, rat; D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists; D018340:Receptors, Adrenergic, alpha-1