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Bioorg Med Chem Lett. 1998 Feb 3;8(3):243-8.

Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo.

Author information

1
Department of Chemical Research, Schering-Plough Research Institute, Kenilworth, New Jersy 07033-0539, USA.

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.

PMID:
9871662
DOI:
10.1016/s0960-894x(98)00020-1
[Indexed for MEDLINE]

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