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Novel heterocycles as selective alpha1-adrenergic receptor antagonists
1The R. W. Johnson Pharmaceutical Research Institute, San Diego, CA 92121, USA. xli@prius.jnj.com
Bioorganic & Medicinal Chemistry Letters
|October 31, 2000
Abstract:
A novel series of aryl piperazine substituted heterocycles has been synthesized and identified as antagonists of the alpha1a-adrenergic receptor (alpha1a-AR), which has been implicated in benign prostatic hyperplasia (BPH). These compounds selectively inhibit binding to the alpha1a-AR with K(i)s as low as 2.1 nM.