Cilnidipine
Cilnidipine is a dihydropyridine that exhibits antihypertensive, vasodilatory, antinociceptive, and nephroprotective activities. Cilnidipine acts as an antagonist at L-type and N-type voltage-gated Ca2+ channels. In subjects with hypertension, cilnidipine decreases blood pressure and urinary albumin excretion. Cilnidipine also increases expression of eNOS ex vivo in thoracic arteries. In animal models of non insulin-dependent diabetes, cilnidipine improves insulin sensitivity, indicating potential anti-diabetic activity as well. This compound inhibits nociception in animal models undergoing the formalin test. Additionally, in vitro, cilnidipine decreases production of AP-1, TGF-β, and fibronectin, inhibiting proliferation of mesangial cells; in similar animal models, cilnidipine inhibits progression of glomerulonephritis.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18851928
| Cas No. |
132203-70-4 |
|---|---|
| Purity |
≥98% |
| Formula |
C27H26N2O7 |
| Formula Wt. |
490.525 |
| IUPAC Name |
3-O-(2-methoxyethyl) 5-O-[(E)-3-phenylprop-2-enyl]2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| Melting Point |
97-99°C |
| Appearance |
Light yellow crystal powder |
Soeki T, Kitani M, Kusunose K, et al. Renoprotective and antioxidant effects of cilnidipine in hypertensive patients. Hypertens Res. 2012 Nov;35(11):1058-62. PMID: 22763473.
Fan L, Yang Q, Xiao XQ, et al. Dual actions of cilnidipine in human internal thoracic artery: inhibition of calcium channels and enhancement of endothelial nitric oxide synthase. J Thorac Cardiovasc Surg. 2011 Apr;141(4):1063-9. PMID: 20599230.
Koganei H, Shoji M, Iwata S. Suppression of formalin-induced nociception by cilnidipine, a voltage-dependent calcium channel blocker. Biol Pharm Bull. 2009 Oct;32(10):1695-700. PMID: 19801830.
Sugiura T, Imai E, Moriyama T, et al. Calcium channel blockers inhibit proliferation and matrix production in rat mesangial cells: possible mechanism of suppression of AP-1 and CREB activities. Nephron. 2000 May;85(1):71-80. PMID: 10773759.
Harada N, Ohnaka M, Sakamoto S, et al. Cilnidipine improves insulin sensitivity in the Otsuka Long-Evans Tokushima fatty rat, a model of spontaneous NIDDM. Cardiovasc Drugs Ther. 1999 Nov;13(6):519-23. PMID: 10686661.
Fan YY, Kohno M, Nakano D, et al. Cilnidipine suppresses podocyte injury and proteinuria in metabolic syndrome rats: possible involvement of N-type calcium channel in podocyte. J Hypertens. 2010 May;28(5):1034-1043. PMID: 20411599.
