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