A recent uroselective alpha(1)-adrenoceptor antagonist, REC15/2739, has been joined with nitrooxy and furoxan NO-donor moieties to give new NO-donor alpha(1)-antagonists. All the compounds studied proved to be potent and selective ligands of human cloned alpha(1a)-receptor subtype. Derivatives 6 and 7 were able to relax the prostatic portion of rat vas deferens contracted by (-)-noradrenaline because of both their alpha(1A)-antagonist and their NO-donor properties.

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm030825uDOI Listing

Publication Analysis

Top Keywords

no-donor alpha1-antagonists
8
potential uroselective
4
no-donor
4
uroselective no-donor
4
alpha1-antagonists uroselective
4
uroselective alpha1-adrenoceptor
4
alpha1-adrenoceptor antagonist
4
antagonist rec15/2739
4
rec15/2739 joined
4
joined nitrooxy
4

Similar Publications

New potential uroselective NO-donor alpha1-antagonists.

J Med Chem

August 2003

Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, via Pietro Giuria 9, 10125 Turin, Italy.

A recent uroselective alpha(1)-adrenoceptor antagonist, REC15/2739, has been joined with nitrooxy and furoxan NO-donor moieties to give new NO-donor alpha(1)-antagonists. All the compounds studied proved to be potent and selective ligands of human cloned alpha(1a)-receptor subtype. Derivatives 6 and 7 were able to relax the prostatic portion of rat vas deferens contracted by (-)-noradrenaline because of both their alpha(1A)-antagonist and their NO-donor properties.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!