Chemical Name:[1S-(1a,2a,5b)]-[5-Methyl-2-(1-methylethyl)cyclohexyl]d
iphenylphosphine oxide
Biological Activity:
Blocker
of IKur ultrarapid delayed rectifier potassium current and KV1.5
channels (IC50 = 0.31 μM for rKV1.5). Displays
selectivity for inhibition of IKur over Ito (8-fold), IK1,
IKr and IKs (20-fold) in native myocytes and selectivity
for rat recombinant KV1.5 over KV3.1 (~ 15-fold).
Increases action potential duration in atrial but not ventricular myocytes and
prevents atrial arrhythmia.
Stumpet al (2005) In vivo
antiarrhythmic and cardiac electrophysiologic effects of a novel
diphenylphosphine oxide IKur blocker
(2-isopropyl-5-methylcyclohexyl) diphenylphosphine oxide. J.Pharmacol.Exp.Ther.
315 1362. Reganet al (2006) In vivo cardiac
electrophysiologic effects of a novel diphenylphosphine oxide IKur
blocker, (2-isopropyl-5-methylcyclohexyl) diphenylphosphine oxide, in rat and
nonhuman primate. J.Pharmacol.Exp.Ther. 316 727. Lagruttaet
al (2006) Novel, potent inhibitors of human Kv1.5 K+ channels
and ultrarapid activating delayed rectifier potassium current. J Pharmacol.
Exp.Ther. 317 1054.
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