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 Citations (Scopus)

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

Fingerprint

Cholinergic Receptors
Muscarinic Receptors
Cerebral Cortex
Muscarinic Antagonists
Binding Sites
himbacine
Ligands
Membranes

Keywords

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

ASJC Scopus subject areas

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

Cite this

Himbacine recognizes a high affinity subtype of M2 muscarinic cholinergic receptors in the rat cerebral cortex. / Wang, Jian xin; Roeske, William R; Wang, Wan; Yamamura, Henry I.

In: Brain Research, Vol. 446, No. 1, 12.04.1988, p. 155-158.

Research output: Contribution to journalArticle

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