Himbacine recognizes a high affinity subtype of M2 muscarinic cholinergic receptors in the rat cerebral cortex

Jian xin Wang, William R. Roeske, Wan Wang, Henry I. Yamamura

Research output: Contribution to journalArticle

18 Scopus citations

Abstract

The in vitro receptor binding properties of a muscarinic antagonist himbacine have been studied in rat cerebral cortical, cardiac and ileal membranes. Himbacine displayed high affinity (KH = 2.94 nM) 19%, and low affinity (KL = 71.2 nM) for the remaining muscarinic receptors in rat cerebral cortex. This high affinity of himbacine agrees with its affinity for the 62% of cerebral cortical [3H]AF-DX 116 binding sites (KH = 2.30 nM). The affinity of himbacine for cardiac receptors (Ki = 9.06 nM) and ileal receptors (Ki = 12.4 nM) was the same. Therefore, himbacine appears to be a high-affinity M2-selective ligand which recognizes a subtype of M2 receptors in the cerebral cortex.

Original languageEnglish (US)
Pages (from-to)155-158
Number of pages4
JournalBrain Research
Volume446
Issue number1
DOIs
StatePublished - Apr 12 1988
Externally publishedYes

Keywords

  • Heart
  • Heterogeneity
  • Himbacine
  • Ileum
  • Muscarinic cholinergic receptor
  • Rat cerebral cortex

ASJC Scopus subject areas

  • Neuroscience(all)
  • Molecular Biology
  • Clinical Neurology
  • Developmental Biology

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