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Vol. 289, Issue 1, 551-558, April 1999
Neurological and Urological Diseases Research, Pharmaceutical
Products Division, Abbott Laboratories, Abbott Park, Illinois
ATP-sensitive K+ (KATP) channels play an
important role in the regulation of smooth muscle membrane potential.
To investigate the properties of KATP channels in guinea
pig urinary bladder smooth muscle cells, fluorescence-based assays were
carried out with the membrane potential-sensitive probe
bis-(1,3-dibutylbarbituric acid)trimethine oxonol
[DiBAC4(3)]. The prototypical channel openers, including
pinacidil, (
)-cromakalim, and diazoxide, elicited
concentration-dependent decreases in membrane potential that were
attenuated by glyburide. Similar responses were evoked by a reduction
in intracellular ATP levels by metabolic inhibition. The observed rank
order potency (EC50) for evoking membrane potential changes
by potassium channel openers, P1075 (53 nM) ~ Bay X 9228 > ()-cromakalim ~ ZD6169 ~ pinacidil > Bay X
9227 ~ ZM244085 > diazoxide (59 µM), showed a good
correlation with that of bladder smooth muscle relaxation, as assessed
by isolated tissue bath studies. The maximal efficacies of
()-cromakalim, pinacidil, Bay X 9228, and ZD6169 were
comparable with the response achieved by the reference activator P1075.
Whole cell currents in bladder smooth muscle cells were increased in both inward and outward directions by P1075 and were reversed by
glyburide to control levels. The molecular composition assessed by
reverse transcriptase-polymerase chain reaction analysis using subunit-specific primers revealed the presence of mRNA for inward rectifying potassium channel (KIR6.2) and sulfonylurea
receptors (SUR)2B and SUR1. The subunit profile together with
pharmacological properties suggests that the KATP channel
in bladder smooth muscle cells could be composed of SUR2B associated
with a single inward rectifier, KIR6.2. In summary, these
studies have characterized the pharmacological profile using
fluorescent imaging plate reader-based membrane potential techniques
and provide evidence for the molecular identity of KATP
channels expressed in guinea pig bladder smooth muscle cells.
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