Maturation of mammalian myocardial muscarinic cholinergic receptors

William R. Roeske, Henry I. Yamamura

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

Abstract

Biochemical alterations of the cardiac muscarinic binding sites have not been correlated with physiological observations. The development of responsiveness to acetylcholine in the fetal mouse heart occurs during the third trimester. We tested the hypothesis that the altered physiological response was related to changes in the muscarinic cholinergic binding site assayed by using the potent antagonist [3H]-quinuclidinyl benzilate (QNB). Analysis of saturation isotherms of specific (atropine displaceable) [3H]-QNB binding gave an apparent dissociation constant (KDapp) of 27 ± 3 (SEM) pM for adult heart. Receptor density increased significantly during the third trimester of pregnancy to 48% of adult, while the KDapp did not change. The increase in receptor density parallels the demonstrated increased responsiveness to acetylcholine.

Original languageEnglish (US)
Pages (from-to)127-132
Number of pages6
JournalLife Sciences
Volume23
Issue number2
DOIs
StatePublished - Jul 10 1978
Externally publishedYes

ASJC Scopus subject areas

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

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