trans-4-Methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo

Article abstract of DOI:10.1016/S0960-894X(98)00020-1

Extensive structural modification of immepyr (+)-2 led to the dsiscovery 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.