Maturation of mammalian myocardial muscarinic cholinergic receptors

William R. Roeske; Henry I. Yamamura

doi:10.1016/0024-3205(78)90260-6

Maturation of mammalian myocardial muscarinic cholinergic receptors

William R. Roeske, Henry I. Yamamura

Research output: Contribution to journal › Article › peer-review

15 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 (K_Dapp) of 27 ± 3 (SEM) pM for adult heart. Receptor density increased significantly during the third trimester of pregnancy to 48% of adult, while the K_Dapp did not change. The increase in receptor density parallels the demonstrated increased responsiveness to acetylcholine.

Original language	English (US)
Pages (from-to)	127-132
Number of pages	6
Journal	Life Sciences
Volume	23
Issue number	2
DOIs	https://doi.org/10.1016/0024-3205(78)90260-6
State	Published - Jul 10 1978

ASJC Scopus subject areas

General Pharmacology, Toxicology and Pharmaceutics
General Biochemistry, Genetics and Molecular Biology

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10.1016/0024-3205(78)90260-6

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title = "Maturation of mammalian myocardial muscarinic cholinergic receptors",

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.",

author = "Roeske, {William R.} and Yamamura, {Henry I.}",

note = "Funding Information: This research was supported by an institutional grant and a Grant-In-Aid from the American Heart Association, Arizona Affiliate, and by U .S .P .H .S . Grants HL-21486 and HL-20984 . Henry I . Yamamura ie a recipient of a U .S .P .H .S . Researc h Scientist Development Award, Type-II (tom-00095) . We gratefully acknowledge the technical assistance of Janet Cohn and the secretarial aeais-tance of Miss Ann Vallefuoco .",

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doi = "10.1016/0024-3205(78)90260-6",

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T1 - Maturation of mammalian myocardial muscarinic cholinergic receptors

AU - Roeske, William R.

AU - Yamamura, Henry I.

N1 - Funding Information: This research was supported by an institutional grant and a Grant-In-Aid from the American Heart Association, Arizona Affiliate, and by U .S .P .H .S . Grants HL-21486 and HL-20984 . Henry I . Yamamura ie a recipient of a U .S .P .H .S . Researc h Scientist Development Award, Type-II (tom-00095) . We gratefully acknowledge the technical assistance of Janet Cohn and the secretarial aeais-tance of Miss Ann Vallefuoco .

PY - 1978/7/10

Y1 - 1978/7/10

N2 - 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.

AB - 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.

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JO - Life Sciences

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Maturation of mammalian myocardial muscarinic cholinergic receptors

Abstract

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