alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines

Novel 2'-heteroaryl-2-(phenoxymethyl)imidazolines have been identified as potent agonists of the cloned human alpha(1)-adrenoceptors in vitro. The nature of the 2'-heteroaryl group can have significant effects on the potency, efficacy, and subtype selectivity in this series. alpha(1A) Subt...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-02, Vol.12 (3), p.471-475
Hauptverfasser:	Bishop, Michael J, Barvian, Kevin A, Berman, Judd, Bigham, Eric C, Garrison, Deanna T, Gobel, Michael J, Hodson, Stephen J, Irving, Paul E, Liacos, James A, Navas, 3rd, Frank, Saussy, David L, Speake, Jason D
Format:	Artikel
Sprache:	eng
Schlagworte:	Adrenergic alpha-1 Receptor Agonists Adrenergic alpha-Agonists - pharmacology Humans Hydrogen Bonding Imidazoles - chemical synthesis Imidazoles - pharmacology Phenyl Ethers - chemical synthesis Phenyl Ethers - pharmacology Receptors, Adrenergic, alpha-1 Recombinant Proteins Structure-Activity Relationship Urinary Incontinence, Stress - prevention & control
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Zusammenfassung:	Novel 2'-heteroaryl-2-(phenoxymethyl)imidazolines have been identified as potent agonists of the cloned human alpha(1)-adrenoceptors in vitro. The nature of the 2'-heteroaryl group can have significant effects on the potency, efficacy, and subtype selectivity in this series. alpha(1A) Subtype selective agonists have been identified.
ISSN:	0960-894X
DOI:	10.1016/S0960-894X(01)00764-8