Amlodipine besylate is an L-type calcium channel protein inhibitor and blocker that contains antihypertensive properties. Amlodipine besylate also displays vasoprotective effects in cardiovascular disease and inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM). Amlodipine besylate has been shown to inhibit proliferation of human vascular smooth muscle cells and epidermoid carcinoma A431 cells (IC50 = 25 μM).
1. Arrowsmith, J.E., et al. 1986. J. Med. Chem. 29: 1696-1702. PMID: 2943898 2. Burges, R.A., et al. 1987. J. Cardiovasc. Pharmacol. 9: 110-119. PMID: 2434785 3. Packer, M., et al. 1996. N. Engl. J. Med. 335: 1107-1114. PMID: 8813041 4. Yoshida, J., et al. 2003. Eur. J. Pharmacol. 472: 23-31. PMID: 12860469 5. Toba, H., et al. 2005 Hypertens. Res. 28: 689-700. PMID: 16392774
Soluble in DMSO (≥20 mg/mL), water (10 mM), chloroform, ethanol (≥14 mg/mL), and methanol.
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527.2° C at 760 mmHg (Predicted)
Ca2+-induced contractions : IC50 = 1.9 nM (depolarized rat aorta); proliferation of human vascular smooth muscle cells and epidermoid carcinoma A431 cells: IC50 = 25 µM; bTREK-1: IC50 = 0.43 µM; 35 mM KCl-induced contractions of pig coronary artery rings: IC50 = 22 nM; 35 mM KCl-induced contractions of human coronary artery rings: IC50 = 21 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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Sathyanarayana RaoSathyanarayana Rao, KN. et al. (PubMed 20593148) tested amlodipine besylate, a L-type calcium channel blocker well known for its anti-hypertensive properties, as a potential anti-convulsant. Found that amlodipine besylate reduced seizures in a concentration dependent manner in inbred albino mice. -SCBT Publication Review
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