Imidazoline compounds inhibit KATP channels in guinea pig ventricular myocytes

Kevin Lee; William J. Groh; T. Anne Blair; James G. Maylie; John P. Adelman

doi:10.1016/0014-2999(95)00525-P

Imidazoline compounds inhibit K_ATP channels in guinea pig ventricular myocytes

Kevin Lee, William J. Groh, T. Anne Blair, James G. Maylie, John P. Adelman

Obstetrics and Gynecology

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

17 Scopus citations

Abstract

Phentolamine and related imidazolines inhibit K_ATP channel activity in the pancreatic β cell. In the present study, the effects of several imidazoline-based compounds were examined upon K_ATP channel activity in guinea pig ventricular myocytes. Phentolamine produced a potent inhibition of K_ATP channel activity when examined in either excised inside-out patches or in the whole-cell configuration. This effect was unrelated to phentolamine's ability to antagonise α-adrenoceptors since the non-selective α-adrenoceptor antagonists, benextramine and phenoxybenzamine, failed to affect channel activity. Furthermore, the α-adrenoceptor agonist clonidine together with several related imidazolines inhibited channel activity. This suggests that imidazoline compounds modulate K_ATP channel activity in guinea pig ventricular myocytes and this may have clinical implications for the use of such agents as hypoglycemic drugs.

Original language	English (US)
Pages (from-to)	309-312
Number of pages	4
Journal	European Journal of Pharmacology
Volume	285
Issue number	3
DOIs	https://doi.org/10.1016/0014-2999(95)00525-P
State	Published - Oct 24 1995

Keywords

(Guinea-pig)
Cardiac myocyte
Imidazoline
K channel

ASJC Scopus subject areas

Pharmacology

Access to Document

10.1016/0014-2999(95)00525-P

Cite this

@article{fa436457ea69481a8a94e7be7f4e5c83,

title = "Imidazoline compounds inhibit KATP channels in guinea pig ventricular myocytes",

abstract = "Phentolamine and related imidazolines inhibit KATP channel activity in the pancreatic β cell. In the present study, the effects of several imidazoline-based compounds were examined upon KATP channel activity in guinea pig ventricular myocytes. Phentolamine produced a potent inhibition of KATP channel activity when examined in either excised inside-out patches or in the whole-cell configuration. This effect was unrelated to phentolamine's ability to antagonise α-adrenoceptors since the non-selective α-adrenoceptor antagonists, benextramine and phenoxybenzamine, failed to affect channel activity. Furthermore, the α-adrenoceptor agonist clonidine together with several related imidazolines inhibited channel activity. This suggests that imidazoline compounds modulate KATP channel activity in guinea pig ventricular myocytes and this may have clinical implications for the use of such agents as hypoglycemic drugs.",

keywords = "(Guinea-pig), Cardiac myocyte, Imidazoline, K channel",

author = "Kevin Lee and Groh, {William J.} and Blair, {T. Anne} and Maylie, {James G.} and Adelman, {John P.}",

note = "Funding Information: We thank Mr. Kevin Gibson for technical support, particularly with myocyte preparations. This work was supported by NIH grants to J.G.M. and J.P.A.",

year = "1995",

month = oct,

day = "24",

doi = "10.1016/0014-2999(95)00525-P",

language = "English (US)",

volume = "285",

pages = "309--312",

journal = "European Journal of Pharmacology",

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T1 - Imidazoline compounds inhibit KATP channels in guinea pig ventricular myocytes

AU - Lee, Kevin

AU - Groh, William J.

AU - Blair, T. Anne

AU - Maylie, James G.

AU - Adelman, John P.

N1 - Funding Information: We thank Mr. Kevin Gibson for technical support, particularly with myocyte preparations. This work was supported by NIH grants to J.G.M. and J.P.A.

PY - 1995/10/24

Y1 - 1995/10/24

N2 - Phentolamine and related imidazolines inhibit KATP channel activity in the pancreatic β cell. In the present study, the effects of several imidazoline-based compounds were examined upon KATP channel activity in guinea pig ventricular myocytes. Phentolamine produced a potent inhibition of KATP channel activity when examined in either excised inside-out patches or in the whole-cell configuration. This effect was unrelated to phentolamine's ability to antagonise α-adrenoceptors since the non-selective α-adrenoceptor antagonists, benextramine and phenoxybenzamine, failed to affect channel activity. Furthermore, the α-adrenoceptor agonist clonidine together with several related imidazolines inhibited channel activity. This suggests that imidazoline compounds modulate KATP channel activity in guinea pig ventricular myocytes and this may have clinical implications for the use of such agents as hypoglycemic drugs.

AB - Phentolamine and related imidazolines inhibit KATP channel activity in the pancreatic β cell. In the present study, the effects of several imidazoline-based compounds were examined upon KATP channel activity in guinea pig ventricular myocytes. Phentolamine produced a potent inhibition of KATP channel activity when examined in either excised inside-out patches or in the whole-cell configuration. This effect was unrelated to phentolamine's ability to antagonise α-adrenoceptors since the non-selective α-adrenoceptor antagonists, benextramine and phenoxybenzamine, failed to affect channel activity. Furthermore, the α-adrenoceptor agonist clonidine together with several related imidazolines inhibited channel activity. This suggests that imidazoline compounds modulate KATP channel activity in guinea pig ventricular myocytes and this may have clinical implications for the use of such agents as hypoglycemic drugs.

KW - (Guinea-pig)

KW - Cardiac myocyte

KW - Imidazoline

KW - K channel

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