Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists

A novel series of arylpiperazines has been synthesized and identified as antagonists of alpha1a adrenergic receptor (alpha1a-AR) implicated in benign prostatic hyperplasia. These compounds selectively bind to membrane bound alpha1a-AR with K(i)s as low as 0.66 nM. As such, these potentially represen...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-05, Vol.10 (10), p.1093-1096
Hauptverfasser:	Li, X, Murray, W V, Jolliffe, L, Pulito, V
Format:	Artikel
Sprache:	eng
Schlagworte:	Adrenergic alpha-1 Receptor Antagonists Adrenergic Antagonists - chemistry Adrenergic Antagonists - metabolism Adrenergic Antagonists - pharmacology Animals Biochemistry - methods Cell Membrane - metabolism COS Cells - metabolism Drug Evaluation, Preclinical - methods Humans In Vitro Techniques Male Muscle Contraction - drug effects Muscle, Smooth - drug effects Piperazine Piperazines - chemistry Piperazines - metabolism Piperazines - pharmacology Piperidines - chemistry Piperidines - metabolism Piperidines - pharmacology Prostate - drug effects Rats Receptors, Adrenergic, alpha-1 - genetics Receptors, Adrenergic, alpha-1 - metabolism Recombinant Proteins - drug effects Recombinant Proteins - genetics Recombinant Proteins - metabolism Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	A novel series of arylpiperazines has been synthesized and identified as antagonists of alpha1a adrenergic receptor (alpha1a-AR) implicated in benign prostatic hyperplasia. These compounds selectively bind to membrane bound alpha1a-AR with K(i)s as low as 0.66 nM. As such, these potentially represent a viable treatment for BPH without the side effects associated with known alpha1-adrenergic antagonists.
ISSN:	0960-894X