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

Authors
  • Shih, N Y
  • Aslanian, R
  • Lupo, A T Jr
  • Orlando, S
  • Piwinski, J J
  • Green, M J
  • Ganguly, A K
  • West, R
  • Tozzi, S
  • Kreutner, W
  • Hey, J A
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Feb 03, 1998
Volume
8
Issue
3
Pages
243–248
Identifiers
PMID: 9871662
Source
Medline
License
Unknown

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.

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