Author/Authors :
Neng-Yang Shih، نويسنده , , Robert Aslanian، نويسنده , , Andrew T. Lupo Jr.، نويسنده , , Steve Orlando، نويسنده , , John J. Piwinski، نويسنده , , Michael J. Green، نويسنده , , Ashit K. Ganguly، نويسنده , , Robert West، نويسنده , , Salvatore Tozzi، نويسنده , , William Kreutner، نويسنده , , John A. Hey، نويسنده ,
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)-α-methylhistamine (+)-1 (H3/H1 RATIO = 17), the standard H3 agonist.
