title: Synthesis and biological activities of 2-[(heteroaryl)methyl]imidazolines.
abstract: A series of 2-[(heteroaryl)methyl]imidazolines was synthesized and tested for their activities at α(1)- and α(2)-adrenoceptors and imidazoline I(1) and I(2) receptors. The most active 2-[(indazol-1-yl)methyl]imidazolines showed high or moderate affinities for α(1)- and α(2)-adrenoceptors. However, their intrinsic activities at α(2A)-adrenoceptors proved to be negligible. A selected 7-chloro derivative behaved as a potent α(1)-adrenoceptor antagonist and exhibited peripherally mediated hypotensive effects in rats.
authors.affiliation: Department of Chemical Technology of Drugs, Medical University of Gdańsk, Al. Gen. J. Hallera 107, Gdańsk 80-416, Poland. js@gumed.edu.pl
authors.forename: Jaroslaw
authors.initials: J
authors.lastname: Saczewski
authors.forename: Alan
authors.initials: A
authors.lastname: Hudson
authors.forename: Mika
authors.initials: M
authors.lastname: Scheinin
authors.forename: Apolonia
authors.initials: A
authors.lastname: Rybczynska
authors.forename: Daqing
authors.initials: D
authors.lastname: Ma
authors.forename: Franciszek
authors.initials: F
authors.lastname: Saczewski
authors.forename: Shayna
authors.initials: S
authors.lastname: Laird
authors.forename: Jonne M
authors.initials: JM
authors.lastname: Laurila
authors.forename: Konrad
authors.initials: K
authors.lastname: Boblewski
authors.forename: Artur
authors.initials: A
authors.lastname: Lehmann
authors.forename: Jianteng
authors.initials: J
authors.lastname: Gu
authors.forename: Helena
authors.initials: H
authors.lastname: Watts
mesh_terms: D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D048288:Imidazolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D018340:Receptors, Adrenergic, alpha-1 / Q000737:chemistry / Q000378:metabolism; D018341:Receptors, Adrenergic, alpha-2 / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000317:Adrenergic alpha-Antagonists; D048288:Imidazolines; D018340:Receptors, Adrenergic, alpha-1; D018341:Receptors, Adrenergic, alpha-2