Description
Clinidipine is a kind of calcium channel blocker. It is a kind of novel calcium antagonist with the blocking effect on both L-type and N-type calcium channels. It is mainly used for the treatment of hypertension. Based on its effect on both N-type and L-type calcium channel, it can dilate both arterioles and venules, further reducing the pressure in the capillary bed. In addition, cilinidipine can attenuate the platelet activation associated with catecholamines.
References
https://www.drugbank.ca/drugs/DB09232
https://en.wikipedia.org/wiki/Cilnidipine
Description
Cilnidipine is a dihydropyridine calcium antagonist introduced for the
treatment of essential and severe hypertension and hypertension associated with
renopathy. Cilnidipine has been demonstrated to exert a potent vasodilating effect by blocking calcium influx via dihydropyridine-sensitive, voltage-dependent calcium
channels. Compared to nifedipine and nicardipine, cilnidipine is superior, especially for
long-term treatment, due to its characteristics of slow onset and long duration with less
cardiodepressant activity. Cilnidipine is reportedly well tolerated with low toxicity.
It may also be useful in ischemic heart disease.
Description
Cilnidipine is a dihydropyridine calcium channel blocker that blocks L- and N-type high-voltage-activated calcium currents in rat hippocampal CA1 pyramidal neurons when used at a concentration of 10 μM. Cilnidipine (3 mg/kg) reduces the pressor response to acute cold stress, as well as mean blood pressure, in spontaneously hypertensive rats. It dose-dependently reduces mean blood pressure and cerebral vascular resistance without affecting cerebral blood flow in anesthetized rats at doses ranging from 3-100 μg/kg. Cilnidipine (100 μg/kg, i.p.) reduces cerebral infarction area in a rat model of focal brain ischemia.
Chemical Properties
Yellow Crystalline Solid
Originator
Fujirebio (Japan)
Uses
Cilnidipine has been used:
- in cell viability assay of pheochromocytoma (nPC12) cells
- in photoirradiation and photodegradation studies
- to understand effect on albuminuria in diabetic nephropathy
Uses
A dihydropyridine calcium channel blocker.
Uses
antihypertensive;dihydropyridine calcium channel blocker
Definition
ChEBI: A diesterified 1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium channel blocker, it is used as an antihypertensive.
brand name
Cinalong;Siscard;Atelec
Biological Activity
Dual L- and N-type calcium channel blocker that displays antihypertensive, sympatholytic and neuroprotective activity. Lowers mean blood pressure and reduces the size of cerebral infarction in the rat model of focal brain ischemia.
Biochem/physiol Actions
Cilnidipine is a slow-acting Ca2+ channel blocker; antihypertensive; vasodilator; dual blocker of L-type voltage-gated Ca2+ channels in vascular smooth muscle and N-type Ca2+ channels in sympathetic nerve terminals that supply blood vessels. Cilnidipine may offer an advantage over nifedipine as the long term intake of the latter has been linked to increased risk of myocardial infarction and mortality in patients with coronary artery disease. Cilnidipine lowers blood pressure, but has less effect on sympathetic activity. Unlike nifedipine, cilnidipine does not inhibit PKC.
References
[1] YOSHINAKA MURAI . Preferential inhibition of L- and N-type calcium channels in the rat hippocampal neurons by cilnidipine[J]. Brain Research, 2000, 854 1: Pages 6-10. DOI:
10.1016/s0006-8993(99)02295-7[2] MASAHIRO HOSONO . Inhibitory Effect of Cilnidipine on Pressor Response to Acute Cold Stress in Spontaneously Hypertensive Rats[J]. Japanese journal of pharmacology, 1995, 69 2: Pages 119-125. DOI:
10.1254/jjp.69.119[3] AKIRA TAKAHARA. Neuroprotective effects of a dual L/N-type Ca(2+) channel blocker cilnidipine in the rat focal brain ischemia model.[J]. Biological & pharmaceutical bulletin, 2004, 27 9: 1388-1391. DOI:
10.1248/bpb.27.1388
