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Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo
N Y Shih1, R Aslanian, A T Lupo
1Department of Chemical Research, Schering-Plough Research Institute, Kenilworth, New Jersy 07033-0539, USA.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
Abstract:
Extensive structural modification of immepyr (+)-2 led to the discovery of trans-4-methyl-3-imidazoyl pyrrolidine (+/-)-3a as a potent and highly selective H3 agonist. The pyrroline (+/-)-3a was resolved, and its (+) enantiomer, Sch 50971 [(+)-3a], showed a greater separation of H3 and H1 activities in vivo (H3/H1 ratio >> 330) than (R)-alpha-methylhistamine (+)-1 (H3/H1 ratio = 17), the standard H3 agonist.