Endothelin receptors in human and guinea-pig gallbladder muscle

Shih Che Huang; Ming Che Lee; Chang Kao Wei; Shih Ming Huang

doi:10.1016/S0167-0115(00)00238-X

Endothelin receptors in human and guinea-pig gallbladder muscle

Shih Che Huang, Ming Che Lee, Chang Kao Wei, Shih Ming Huang

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

24 Citations (Scopus)

Abstract

We measured contraction of muscle strips caused by endothelin (ET) isopeptides and binding of ¹²⁵I-ET-1 to muscle cell membranes prepared from human and guinea-pig gallbladders. Visualization of ¹²⁵I-ET-1 binding sites in tissue was performed by autoradiography. Results in human were similar to those in guinea-pig. ET-1 caused tetrodotoxin and atropine-insensitive contraction. The relative potencies for ET isopeptides to cause contraction were ET-1 = ET-2 > ET-3. ET-1 caused contraction was only slightly inhibited by BQ-123 (potent ET_A receptor antagonist) and not by BQ-788 (potent ET_B receptor antagonist). It was inhibited by the combination of both. Autoradiography localized ¹²⁵I-ET-1 binding to the smooth muscle layer. Binding of ¹²⁵I-ET-1 to muscle cell membranes was saturable and specific. Analysis of dose-inhibition curves demonstrated the presence of two classes of receptors. One class (ET_A receptor) had a high affinity for ET-1 and ET-2 but a low affinity for ET-3, and the other (ET_B receptor) a high affinity for ET-1, ET-2 and ET-3. These results demonstrate that similar to guinea-pig, human gallbladder possesses both ET_A and ET_B receptors cooperating to mediate muscle contraction.

Original language	English
Pages (from-to)	145-153
Number of pages	9
Journal	Regulatory Peptides
Volume	98
Issue number	3
DOIs	https://doi.org/10.1016/S0167-0115(00)00238-X
Publication status	Published - Apr 20 2001
Externally published	Yes

Keywords

Autoradiography
Binding
Contraction
ET
Motility

ASJC Scopus subject areas

Biochemistry
Physiology
Endocrinology
Clinical Biochemistry
Cellular and Molecular Neuroscience

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10.1016/S0167-0115(00)00238-X

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@article{d2366b45a8694b0dab54255231584124,

title = "Endothelin receptors in human and guinea-pig gallbladder muscle",

abstract = "We measured contraction of muscle strips caused by endothelin (ET) isopeptides and binding of 125I-ET-1 to muscle cell membranes prepared from human and guinea-pig gallbladders. Visualization of 125I-ET-1 binding sites in tissue was performed by autoradiography. Results in human were similar to those in guinea-pig. ET-1 caused tetrodotoxin and atropine-insensitive contraction. The relative potencies for ET isopeptides to cause contraction were ET-1 = ET-2 > ET-3. ET-1 caused contraction was only slightly inhibited by BQ-123 (potent ETA receptor antagonist) and not by BQ-788 (potent ETB receptor antagonist). It was inhibited by the combination of both. Autoradiography localized 125I-ET-1 binding to the smooth muscle layer. Binding of 125I-ET-1 to muscle cell membranes was saturable and specific. Analysis of dose-inhibition curves demonstrated the presence of two classes of receptors. One class (ETA receptor) had a high affinity for ET-1 and ET-2 but a low affinity for ET-3, and the other (ETB receptor) a high affinity for ET-1, ET-2 and ET-3. These results demonstrate that similar to guinea-pig, human gallbladder possesses both ETA and ETB receptors cooperating to mediate muscle contraction.",

keywords = "Autoradiography, Binding, Contraction, ET, Motility",

author = "Huang, {Shih Che} and Lee, {Ming Che} and Wei, {Chang Kao} and Huang, {Shih Ming}",

note = "Funding Information: This work was supported by National Science Council of Taiwan, China (NSC grant 89-2314-B-303-006) and by Tzu Chi University. We thank Dr Yung-Hsiang Hsu, Department of Pathology, Tzu Chi General Hospital, for help with autoradiographic studies. The authors would like to acknowledge Yu-Jen Chen, Keng-Hsien Kuo and Chia-Yi Wang for excellent technical assistance.",

year = "2001",

month = apr,

day = "20",

doi = "10.1016/S0167-0115(00)00238-X",

language = "English",

volume = "98",

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T1 - Endothelin receptors in human and guinea-pig gallbladder muscle

AU - Huang, Shih Che

AU - Lee, Ming Che

AU - Wei, Chang Kao

AU - Huang, Shih Ming

N1 - Funding Information: This work was supported by National Science Council of Taiwan, China (NSC grant 89-2314-B-303-006) and by Tzu Chi University. We thank Dr Yung-Hsiang Hsu, Department of Pathology, Tzu Chi General Hospital, for help with autoradiographic studies. The authors would like to acknowledge Yu-Jen Chen, Keng-Hsien Kuo and Chia-Yi Wang for excellent technical assistance.

PY - 2001/4/20

Y1 - 2001/4/20

N2 - We measured contraction of muscle strips caused by endothelin (ET) isopeptides and binding of 125I-ET-1 to muscle cell membranes prepared from human and guinea-pig gallbladders. Visualization of 125I-ET-1 binding sites in tissue was performed by autoradiography. Results in human were similar to those in guinea-pig. ET-1 caused tetrodotoxin and atropine-insensitive contraction. The relative potencies for ET isopeptides to cause contraction were ET-1 = ET-2 > ET-3. ET-1 caused contraction was only slightly inhibited by BQ-123 (potent ETA receptor antagonist) and not by BQ-788 (potent ETB receptor antagonist). It was inhibited by the combination of both. Autoradiography localized 125I-ET-1 binding to the smooth muscle layer. Binding of 125I-ET-1 to muscle cell membranes was saturable and specific. Analysis of dose-inhibition curves demonstrated the presence of two classes of receptors. One class (ETA receptor) had a high affinity for ET-1 and ET-2 but a low affinity for ET-3, and the other (ETB receptor) a high affinity for ET-1, ET-2 and ET-3. These results demonstrate that similar to guinea-pig, human gallbladder possesses both ETA and ETB receptors cooperating to mediate muscle contraction.

AB - We measured contraction of muscle strips caused by endothelin (ET) isopeptides and binding of 125I-ET-1 to muscle cell membranes prepared from human and guinea-pig gallbladders. Visualization of 125I-ET-1 binding sites in tissue was performed by autoradiography. Results in human were similar to those in guinea-pig. ET-1 caused tetrodotoxin and atropine-insensitive contraction. The relative potencies for ET isopeptides to cause contraction were ET-1 = ET-2 > ET-3. ET-1 caused contraction was only slightly inhibited by BQ-123 (potent ETA receptor antagonist) and not by BQ-788 (potent ETB receptor antagonist). It was inhibited by the combination of both. Autoradiography localized 125I-ET-1 binding to the smooth muscle layer. Binding of 125I-ET-1 to muscle cell membranes was saturable and specific. Analysis of dose-inhibition curves demonstrated the presence of two classes of receptors. One class (ETA receptor) had a high affinity for ET-1 and ET-2 but a low affinity for ET-3, and the other (ETB receptor) a high affinity for ET-1, ET-2 and ET-3. These results demonstrate that similar to guinea-pig, human gallbladder possesses both ETA and ETB receptors cooperating to mediate muscle contraction.

KW - Autoradiography

KW - Binding

KW - Contraction

KW - ET

KW - Motility

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DO - 10.1016/S0167-0115(00)00238-X

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VL - 98

SP - 145

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JO - Regulatory Peptides

JF - Regulatory Peptides

SN - 0167-0115

IS - 3

ER -

Endothelin receptors in human and guinea-pig gallbladder muscle

Abstract

Keywords

ASJC Scopus subject areas

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