Striatal muscarinic receptors: Regulation by dopaminergic agonists

Frederick J. Ehlert, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

The effects of apomorphine on the binding properties of striatal muscarinic receptors were investigated using the specific muscarinic antagonist, [3H](-)3-quinuclidinyl benzilate ([3H](-)QNB). When binding measurements were made in 50 mM sodium/HEPES buffer, pH 7.4, containing Mg+2, the binding of [3H](-)QNB was consistent with the presence of two binding sites; 57% of the sites had a high affinity dissociation constant of 0.030 nM whereas the remaining sites had a low affinity dissociation constant of 0.64 nM. Apomorphine (1.0 μM) enhanced the binding of [3H](-)QNB by an apparent conversion of low to high affinity sites. A variety of other agents were screened for their ability to enhance [3H](-)QNB binding, and a pattern generally consistent with a dopaminergic effect was observed although some evidence for a β-adrenergic effect was demonstrable. The potent neuroleptics haloperidol, spiperone and sulpiride failed to antagonize the apomorphine enhancement of [3H](-)QNB binding as well as some adrenergic antagonists. However, the potent inhibitors of the dopamine-sensitive adenylate cyclase, α-flupenthixol and fluphenazine, specifically blocked the apomorphine enhancement of [3H](-)QNB binding with Ki values of approximately 0.1 μM.

Original languageEnglish (US)
Pages (from-to)2441-2448
Number of pages8
JournalLife Sciences
Volume28
Issue number21
DOIs
StatePublished - May 21 1981

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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