AM 92016 hydrochloride |
Catalog No.GC10943 |
El clorhidrato AM 92016 es un bloqueador específico de la corriente rectificadora de potasio (IK).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 133229-11-5
Sample solution is provided at 25 µL, 10mM.
AM 92016 hydrochloride is a specific inhibitor of delayed rectifier potassium current [1].
Potassium channel is an ion channel and acts to reset the resting potential and shapes the action potential. Delayed rectifier potassium channel (IK) is activated by the influx of Na+ and discharges K+, which repolarizes the membrane. IK restricts the duration of the nerve impulse.
AM 92016 hydrochloride is a specific iK inhibitor. In guinea-pig and rabbit ventricular cells, AM 92016 significantly increased action potential duration with 20% and 90% repolarization levels, respectively. Also, AM 92016 (1 μM) inhibited IK activated by step depolarizations in a time-dependent way [1]. In rabbit sino-atrial node cells, AM 92016 (50 nM) significantly inhibited IK with IC50 value of 40 nM in a concentration-dependent way [2]. In vascular smooth muscle cells (VSMC), AM92016 hydrochloride inhibited NO-induced ERK1/2 dephosphorylation [3].
In guinea-pigs, AM 92016 (1-5 mg/kg) significantly increased heart rate, left ventricular systolic pressure, systolic arterial blood pressure and the contractile index dp dtmax. AM 92016 exhibited proarrhythmic activity [4].
References:
[1]. Connors SP, Gill EW, Terrar DA. Actions and mechanisms of action of novel analogues of sotalol on guinea-pig and rabbit ventricular cells. Br J Pharmacol, 1992, 106(4): 958-965.
[2]. Lei M, Brown HF. Inhibition by Compound II, a sotalol analogue, of delayed rectifier current (iK) in rabbit isolated sino-atrial node cells. Naunyn Schmiedebergs Arch Pharmacol, 1998, 357(3): 260-267.
[3]. Palen DI, Belmadani S, Lucchesi PA, et al. Role of SHP-1, Kv.1.2, and cGMP in nitric oxide-induced ERK1/2 MAP kinase dephosphorylation in rat vascular smooth muscle cells. Cardiovasc Res, 2005, 68(2): 268-277.
[4]. Hagerty MJ, Wainwright CL, Kane KA. The in-vivo cardiovascular effects of a putative class III anti-arrhythmic drug, AM 92016. J Pharm Pharmacol, 1996, 48(4): 417-421.
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