Muscarinic receptors in rat uterus

Jocelyn N. Pennefather; Tracey A. Gillman; Frederick Mitchelson

doi:10.1016/0014-2999(94)90745-5

Muscarinic receptors in rat uterus

Jocelyn N. Pennefather, Tracey A. Gillman, Frederick Mitchelson

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

26 Citations (Scopus)

Abstract

The aim of this study was to characterise the muscarinic receptor present in the uterus of the virgin rat. Homogenate binding studies were undertaken using [³H]quinuclidinyl benzilate as the radioligand and atropine (10 μM) to determine non-specific binding. [³H]Quinuclidinyl benzilate binding was saturable with a K_d of 63 pM and a B_max of 3 fmol/mg protein. The pK_i values obtained using antagonists with high affinity for differing muscarinic receptor subtypes were pirenzepine, 6.2; hexahydrosiladifenidol, 6.9; AF-DX 116 (11-[[2-[(diethylamino)methyl]-1-piperidinyl]-acetyl]5, 11-dihydro-6H-pyrido[2,3-b] [1,4]benzodiazepine-6-one), 7.0; and himbacine, 7.8. These findings suggest that muscarinic M₂ receptors are present in rat uterus.

Original language	English
Pages (from-to)	297-300
Number of pages	4
Journal	European Journal of Pharmacology
Volume	262
Issue number	3
DOIs	https://doi.org/10.1016/0014-2999(94)90745-5
Publication status	Published - 12 Sept 1994

Keywords

(Rat)
Binding study
Muscarinic M receptor
Selective antagonist
Uterus
[H]Quinuclidinyl benzilate

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10.1016/0014-2999(94)90745-5

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title = "Muscarinic receptors in rat uterus",

abstract = "The aim of this study was to characterise the muscarinic receptor present in the uterus of the virgin rat. Homogenate binding studies were undertaken using [3H]quinuclidinyl benzilate as the radioligand and atropine (10 μM) to determine non-specific binding. [3H]Quinuclidinyl benzilate binding was saturable with a Kd of 63 pM and a Bmax of 3 fmol/mg protein. The pKi values obtained using antagonists with high affinity for differing muscarinic receptor subtypes were pirenzepine, 6.2; hexahydrosiladifenidol, 6.9; AF-DX 116 (11-[[2-[(diethylamino)methyl]-1-piperidinyl]-acetyl]5, 11-dihydro-6H-pyrido[2,3-b] [1,4]benzodiazepine-6-one), 7.0; and himbacine, 7.8. These findings suggest that muscarinic M2 receptors are present in rat uterus.",

keywords = "(Rat), Binding study, Muscarinic M receptor, Selective antagonist, Uterus, [H]Quinuclidinyl benzilate",

author = "Pennefather, {Jocelyn N.} and Gillman, {Tracey A.} and Frederick Mitchelson",

year = "1994",

month = sep,

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doi = "10.1016/0014-2999(94)90745-5",

language = "English",

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T1 - Muscarinic receptors in rat uterus

AU - Pennefather, Jocelyn N.

AU - Gillman, Tracey A.

AU - Mitchelson, Frederick

PY - 1994/9/12

Y1 - 1994/9/12

N2 - The aim of this study was to characterise the muscarinic receptor present in the uterus of the virgin rat. Homogenate binding studies were undertaken using [3H]quinuclidinyl benzilate as the radioligand and atropine (10 μM) to determine non-specific binding. [3H]Quinuclidinyl benzilate binding was saturable with a Kd of 63 pM and a Bmax of 3 fmol/mg protein. The pKi values obtained using antagonists with high affinity for differing muscarinic receptor subtypes were pirenzepine, 6.2; hexahydrosiladifenidol, 6.9; AF-DX 116 (11-[[2-[(diethylamino)methyl]-1-piperidinyl]-acetyl]5, 11-dihydro-6H-pyrido[2,3-b] [1,4]benzodiazepine-6-one), 7.0; and himbacine, 7.8. These findings suggest that muscarinic M2 receptors are present in rat uterus.

AB - The aim of this study was to characterise the muscarinic receptor present in the uterus of the virgin rat. Homogenate binding studies were undertaken using [3H]quinuclidinyl benzilate as the radioligand and atropine (10 μM) to determine non-specific binding. [3H]Quinuclidinyl benzilate binding was saturable with a Kd of 63 pM and a Bmax of 3 fmol/mg protein. The pKi values obtained using antagonists with high affinity for differing muscarinic receptor subtypes were pirenzepine, 6.2; hexahydrosiladifenidol, 6.9; AF-DX 116 (11-[[2-[(diethylamino)methyl]-1-piperidinyl]-acetyl]5, 11-dihydro-6H-pyrido[2,3-b] [1,4]benzodiazepine-6-one), 7.0; and himbacine, 7.8. These findings suggest that muscarinic M2 receptors are present in rat uterus.

KW - (Rat)

KW - Binding study

KW - Muscarinic M receptor

KW - Selective antagonist

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KW - [H]Quinuclidinyl benzilate

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JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 3

ER -

Muscarinic receptors in rat uterus

Abstract

Keywords

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