[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

165 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

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

Access to Document

10.1016/0024-3205(82)90041-8

Cite this

@article{5c28596e02144fdf8ecb8a9729fd3cef,

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.",

year = "1982",

month = nov,

day = "1",

doi = "10.1016/0024-3205(82)90041-8",

language = "English (US)",

volume = "31",

pages = "2019--2023",

journal = "Life Sciences",

issn = "0024-3205",

publisher = "Elsevier Inc.",

number = "18",

}

TY - JOUR

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

AU - Watson, Mark

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.

UR - https://www.scopus.com/pages/publications/0020333849

UR - https://www.scopus.com/pages/publications/0020333849#tab=citedBy

U2 - 10.1016/0024-3205(82)90041-8

DO - 10.1016/0024-3205(82)90041-8

M3 - Article

C2 - 6897437

AN - SCOPUS:0020333849

SN - 0024-3205

VL - 31

SP - 2019

EP - 2023

JO - Life Sciences

JF - Life Sciences

IS - 18

ER -

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

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this