[3H] pirenzepine selectively identifies a high affinity population of muscarinic cholinergic receptors in the rat cerebral cortex

Mark Watson; William R. Roeske; Henry I. Yamamura

doi:10.1016/0024-3205(82)90041-8

[³H] pirenzepine selectively identifies a high affinity population of muscarinic cholinergic receptors in the rat cerebral cortex

Mark Watson, William R. Roeske, Henry I. Yamamura

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

161 Scopus citations

Abstract

The specific binding of [³H] pirenzepine was investigated in homogenates of rat cerebral cortex, cerebellar cortex, and heart. Specific binding of [³H] pirenzepine in the cerebral cortex as defined by displacement with atropine sulfate (1μM) was of high affinity (K_d = 4-10 nM, receptor density = 1.06 pmoles/mg protein), stereoselective, and competitive with drugs specific for the muscarinic receptor. In contrast, few [³H] pirenzepine binding sites were demonstrated in cerebellar and heart homogenates.

Original language	English (US)
Pages (from-to)	2019-2023
Number of pages	5
Journal	Life Sciences
Volume	31
Issue number	18
DOIs	https://doi.org/10.1016/0024-3205(82)90041-8
State	Published - Nov 1 1982

ASJC Scopus subject areas

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

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10.1016/0024-3205(82)90041-8

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title = "[3H] pirenzepine selectively identifies a high affinity population of muscarinic cholinergic receptors in the rat cerebral cortex",

abstract = "The specific binding of [3H] pirenzepine was investigated in homogenates of rat cerebral cortex, cerebellar cortex, and heart. Specific binding of [3H] pirenzepine in the cerebral cortex as defined by displacement with atropine sulfate (1μM) was of high affinity (Kd = 4-10 nM, receptor density = 1.06 pmoles/mg protein), stereoselective, and competitive with drugs specific for the muscarinic receptor. In contrast, few [3H] pirenzepine binding sites were demonstrated in cerebellar and heart homogenates.",

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

note = "Funding Information: Portions of this study was supported in part by USPHS grants MH-30626, MH-27257, and Program Project Grant HL 20984, a Research Scientist Development Award Type II (MH-O0095) from the National Institute of Mental Health to H.I. Yamamura, and a Research Scientist Development Award (HL-00776) from the National Heart, Lung, and Blood Institute to W.R. Roeske. We thank Ms. Terry Austin for her secretarial assistance.",

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T1 - [3H] pirenzepine selectively identifies a high affinity population of muscarinic cholinergic receptors in the rat cerebral cortex

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AU - Roeske, William R.

AU - Yamamura, Henry I.

N1 - Funding Information: Portions of this study was supported in part by USPHS grants MH-30626, MH-27257, and Program Project Grant HL 20984, a Research Scientist Development Award Type II (MH-O0095) from the National Institute of Mental Health to H.I. Yamamura, and a Research Scientist Development Award (HL-00776) from the National Heart, Lung, and Blood Institute to W.R. Roeske. We thank Ms. Terry Austin for her secretarial assistance.

PY - 1982/11/1

Y1 - 1982/11/1

N2 - The specific binding of [3H] pirenzepine was investigated in homogenates of rat cerebral cortex, cerebellar cortex, and heart. Specific binding of [3H] pirenzepine in the cerebral cortex as defined by displacement with atropine sulfate (1μM) was of high affinity (Kd = 4-10 nM, receptor density = 1.06 pmoles/mg protein), stereoselective, and competitive with drugs specific for the muscarinic receptor. In contrast, few [3H] pirenzepine binding sites were demonstrated in cerebellar and heart homogenates.

AB - The specific binding of [3H] pirenzepine was investigated in homogenates of rat cerebral cortex, cerebellar cortex, and heart. Specific binding of [3H] pirenzepine in the cerebral cortex as defined by displacement with atropine sulfate (1μM) was of high affinity (Kd = 4-10 nM, receptor density = 1.06 pmoles/mg protein), stereoselective, and competitive with drugs specific for the muscarinic receptor. In contrast, few [3H] pirenzepine binding sites were demonstrated in cerebellar and heart homogenates.

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[³H] pirenzepine selectively identifies a high affinity population of muscarinic cholinergic receptors in the rat cerebral cortex

Abstract

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