- Furukawa, T. et al. (1999) J. Pharmacol. Exp. Ther. 291, 464.
- Alomone Labs Cilnidipine blocks L-type CaV channel currents expressed in Xenopus oocytes.A. Time course of CaV1.2 (co-expressed with α2δ1 and β1 auxiliary subunits) current, elicited by 100 ms voltage ramp from holding potential of -100 mV to +50 mV, delivered every 10 seconds. Application of 10 µM Cilnidipine (#C-135) inhibits the current amplitude and modifies activation (see panel B. periods of application are indicated by the horizontal bars). B. Representative current traces before and during application of 10 µM Cilnidipine as indicated.
Cilnidipine (CIL) is a potent slow-acting, anti-sympathetic drug that inhibits N-type (IC50 = 200 nM) and L-type (IC50 = 100 nM) Ca2+ channels and thus alleviates hypertension occurrences. CIL is essentially a dihydropyridine with slow onset and long-term vasodilation effects. It is considered to be a "fourth generation" anti-hypertension drug, effective both in vivo and in vitro1,2-4.
In vivo studies have demonstrated CIL to be helpful in mitigating long QT syndrome in a canine model and to reduce ischemic cardiac norepinephrine levels in rabbit model of cardiac infraction. Clinical trials have shown that CIL is highly effective in cases of severe hypertension, that it improves left ventricular function, and is effective in combating hypertension5-8.