The Pharmacology of ATP-Sensitive Potassium Channels

The Pharmacology of ATP-Sensitive Potassium Channels A potassium (K) channel that was inhibited by physiological (f1M) concen­ was first described in the heart ( l). Subsequently, similar K -channels all with trations of intracellular ATP ([ATP]i) and that opened as [ATP]i decreased unitary conductances in the range of skeletal muscle (2_5).1 Such channels constitute what are classically described high K+ conditions) were also found to exist in insulin-secreting cells and in as ATP-sensitive K-channels and were termed Type 1 by Ashcroft & Ashcroft 40-80 pS (measured under symmetrical them is defined as IK(ATP) . Type 1 KATP channels are essentially calcium- and voltage-independent, K+ -selective, and are half-maximally inhibited by [ATP]i in the range (6). In this review they are designated KATP and the current flowing through pharmacological feature is their inhibition by agents like tolbutamide and Types 2, glyburide . Other ATP-sensitive K-channels exist and these were designated 10-100 fJ.M. They exhibit inward rectification and a key calcium and to the inhibitory effects of [ATP] i , but also in their selectivity for potassium and their susceptibility to pharmacological modulation. 3, 4, and 5 (6). Such channels vary not only in their sensitivity to lUnitary conductances are usually measured under quasi-physiological [ K+] http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Annual Review of Pharmacology and Toxicology Annual Reviews

The Pharmacology of ATP-Sensitive Potassium Channels

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Publisher
Annual Reviews
Copyright
Copyright 1993 Annual Reviews. All rights reserved
Subject
Review Articles
ISSN
0362-1642
eISSN
1545-4304
D.O.I.
10.1146/annurev.pa.33.040193.003121
Publisher site
See Article on Publisher Site

Abstract

A potassium (K) channel that was inhibited by physiological (f1M) concen­ was first described in the heart ( l). Subsequently, similar K -channels all with trations of intracellular ATP ([ATP]i) and that opened as [ATP]i decreased unitary conductances in the range of skeletal muscle (2_5).1 Such channels constitute what are classically described high K+ conditions) were also found to exist in insulin-secreting cells and in as ATP-sensitive K-channels and were termed Type 1 by Ashcroft & Ashcroft 40-80 pS (measured under symmetrical them is defined as IK(ATP) . Type 1 KATP channels are essentially calcium- and voltage-independent, K+ -selective, and are half-maximally inhibited by [ATP]i in the range (6). In this review they are designated KATP and the current flowing through pharmacological feature is their inhibition by agents like tolbutamide and Types 2, glyburide . Other ATP-sensitive K-channels exist and these were designated 10-100 fJ.M. They exhibit inward rectification and a key calcium and to the inhibitory effects of [ATP] i , but also in their selectivity for potassium and their susceptibility to pharmacological modulation. 3, 4, and 5 (6). Such channels vary not only in their sensitivity to lUnitary conductances are usually measured under quasi-physiological [ K+]

Journal

Annual Review of Pharmacology and ToxicologyAnnual Reviews

Published: Apr 1, 1993

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