Heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116

John W. Bloom; Marilyn Halonen; Norma A. Seaver; Henry I. Yamamura

doi:10.1016/0024-3205(87)90226-8

Heterogeneity of the M₁ muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116

John W. Bloom, Marilyn Halonen, Norma A. Seaver, Henry I. Yamamura

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

22 Scopus citations

Abstract

Recent studies have demonstrated that the majority of muscarinic receptors in rabbit peripheral lung homogenates bind pirenzepine with high affinity (putative M₁ subtype). In experiments of AF-DX 116 inhibiting [³H](-)quinuclidinyl benzilate or [³H]pirenzepine, we found similar inhibitory constants for AF-DX 116 binding in rat heart and rabbit peripheral lung that were 4-fold smaller (i.e. of higher affinity) than the inhibitory constant for rat cerebral cortex. This result demonstrate heterogeneity of the M₁ muscarinic receptor subtype between peripheral lung and cerebral cortex.

Original language	English (US)
Pages (from-to)	491-496
Number of pages	6
Journal	Life Sciences
Volume	41
Issue number	4
DOIs	https://doi.org/10.1016/0024-3205(87)90226-8
State	Published - Jul 27 1987

ASJC Scopus subject areas

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

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title = "Heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116",

abstract = "Recent studies have demonstrated that the majority of muscarinic receptors in rabbit peripheral lung homogenates bind pirenzepine with high affinity (putative M1 subtype). In experiments of AF-DX 116 inhibiting [3H](-)quinuclidinyl benzilate or [3H]pirenzepine, we found similar inhibitory constants for AF-DX 116 binding in rat heart and rabbit peripheral lung that were 4-fold smaller (i.e. of higher affinity) than the inhibitory constant for rat cerebral cortex. This result demonstrate heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex.",

author = "Bloom, {John W.} and Marilyn Halonen and Seaver, {Norma A.} and Yamamura, {Henry I.}",

note = "Funding Information: We thank Lucia Tobin for technical assistance and Mrs. Sandra Testa for secretarial assistance. This work was supported in part by NIH grant HL 31219 and a grant from the Flinn Foundation. J.W. Bloom is a recipient of Pulmonary Academic Award from NHLBI (HL 00838). H.I. Yamamura is a recipient of a U.S. Public Health Service Research Scientist Development Award, Type II from National Institute of Mental Health (MH-O0095).",

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doi = "10.1016/0024-3205(87)90226-8",

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T1 - Heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116

AU - Bloom, John W.

AU - Halonen, Marilyn

AU - Seaver, Norma A.

AU - Yamamura, Henry I.

N1 - Funding Information: We thank Lucia Tobin for technical assistance and Mrs. Sandra Testa for secretarial assistance. This work was supported in part by NIH grant HL 31219 and a grant from the Flinn Foundation. J.W. Bloom is a recipient of Pulmonary Academic Award from NHLBI (HL 00838). H.I. Yamamura is a recipient of a U.S. Public Health Service Research Scientist Development Award, Type II from National Institute of Mental Health (MH-O0095).

PY - 1987/7/27

Y1 - 1987/7/27

N2 - Recent studies have demonstrated that the majority of muscarinic receptors in rabbit peripheral lung homogenates bind pirenzepine with high affinity (putative M1 subtype). In experiments of AF-DX 116 inhibiting [3H](-)quinuclidinyl benzilate or [3H]pirenzepine, we found similar inhibitory constants for AF-DX 116 binding in rat heart and rabbit peripheral lung that were 4-fold smaller (i.e. of higher affinity) than the inhibitory constant for rat cerebral cortex. This result demonstrate heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex.

AB - Recent studies have demonstrated that the majority of muscarinic receptors in rabbit peripheral lung homogenates bind pirenzepine with high affinity (putative M1 subtype). In experiments of AF-DX 116 inhibiting [3H](-)quinuclidinyl benzilate or [3H]pirenzepine, we found similar inhibitory constants for AF-DX 116 binding in rat heart and rabbit peripheral lung that were 4-fold smaller (i.e. of higher affinity) than the inhibitory constant for rat cerebral cortex. This result demonstrate heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex.

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Heterogeneity of the M₁ muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116

Abstract

ASJC Scopus subject areas

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