Characterization of muscarinic acetylcholine receptors in human labial salivary glands

Lin Mei; William R. Roeske; Kenneth T. Izutsu; Henry I. Yamamura

doi:10.1016/0014-2999(90)90032-2

Characterization of muscarinic acetylcholine receptors in human labial salivary glands

Lin Mei, William R. Roeske, Kenneth T. Izutsu, Henry I. Yamamura

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

28 Scopus citations

Abstract

Muscarinic acetylcholine receptors were studied in human labial salivary glands with (-)-[³H]MQNB. The radioligand bound with a K_d value of 150 pM. The density of muscarinic receptors was 220 fmol/mg protein. Most muscarinic antagonists bound to a homogenous population of muscarinic receptors in this tissue. However, the inhibition curves of pirenzepine had a Hill slope of 0.57 and could be analyzed by a two site model. These results suggest that the muscarinic receptors in human labial salivary glands are a mixture of M₁ and M₃ types.

Original language	English (US)
Pages (from-to)	367-370
Number of pages	4
Journal	European Journal of Pharmacology
Volume	176
Issue number	3
DOIs	https://doi.org/10.1016/0014-2999(90)90032-2
State	Published - Feb 13 1990
Externally published	Yes

Keywords

Labial salivary gland (human)
Muscarinic receptor antagonists
Muscarinic receptor subtypes

ASJC Scopus subject areas

Pharmacology

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10.1016/0014-2999(90)90032-2

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title = "Characterization of muscarinic acetylcholine receptors in human labial salivary glands",

abstract = "Muscarinic acetylcholine receptors were studied in human labial salivary glands with (-)-[3H]MQNB. The radioligand bound with a Kd value of 150 pM. The density of muscarinic receptors was 220 fmol/mg protein. Most muscarinic antagonists bound to a homogenous population of muscarinic receptors in this tissue. However, the inhibition curves of pirenzepine had a Hill slope of 0.57 and could be analyzed by a two site model. These results suggest that the muscarinic receptors in human labial salivary glands are a mixture of M1 and M3 types.",

keywords = "Labial salivary gland (human), Muscarinic receptor antagonists, Muscarinic receptor subtypes",

author = "Lin Mei and Roeske, {William R.} and Izutsu, {Kenneth T.} and Yamamura, {Henry I.}",

note = "Funding Information: This work was supported in part by U.S. Public Health Service Grants HL-20984, DK-36289 and DK-35975. The authors would like to thank Ms. Pam Davis for secretarial services.",

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doi = "10.1016/0014-2999(90)90032-2",

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AU - Mei, Lin

AU - Roeske, William R.

AU - Izutsu, Kenneth T.

AU - Yamamura, Henry I.

N1 - Funding Information: This work was supported in part by U.S. Public Health Service Grants HL-20984, DK-36289 and DK-35975. The authors would like to thank Ms. Pam Davis for secretarial services.

PY - 1990/2/13

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N2 - Muscarinic acetylcholine receptors were studied in human labial salivary glands with (-)-[3H]MQNB. The radioligand bound with a Kd value of 150 pM. The density of muscarinic receptors was 220 fmol/mg protein. Most muscarinic antagonists bound to a homogenous population of muscarinic receptors in this tissue. However, the inhibition curves of pirenzepine had a Hill slope of 0.57 and could be analyzed by a two site model. These results suggest that the muscarinic receptors in human labial salivary glands are a mixture of M1 and M3 types.

AB - Muscarinic acetylcholine receptors were studied in human labial salivary glands with (-)-[3H]MQNB. The radioligand bound with a Kd value of 150 pM. The density of muscarinic receptors was 220 fmol/mg protein. Most muscarinic antagonists bound to a homogenous population of muscarinic receptors in this tissue. However, the inhibition curves of pirenzepine had a Hill slope of 0.57 and could be analyzed by a two site model. These results suggest that the muscarinic receptors in human labial salivary glands are a mixture of M1 and M3 types.

KW - Labial salivary gland (human)

KW - Muscarinic receptor antagonists

KW - Muscarinic receptor subtypes

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Characterization of muscarinic acetylcholine receptors in human labial salivary glands

Abstract

Keywords

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