Cilnidipine

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 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.

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.

Chemical Properties

Yellow Crystalline Solid

Originator

Fujirebio (Japan)

Uses

A dihydropyridine calcium channel blocker.

Uses

antihypertensive;dihydropyridine calcium channel blocker

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

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.

storage

+4°C

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