Reference

Antihypertensive effects of amlodipine besylate and its new salts

Antihypertensive effects of amlodipine besylate and its new salts. Lee, Byung Ho; Seo, Ho Won; Kim, Maeng Sup (Medicinal Science Division, Korea Research Institute of Chemical Technology, Taejon 305-343, S. Korea). Journal of Applied Pharmacology, 11(2), 133-138 (Korean) 2003 Korean Society of Applied Pharmacology. 111470-99-6 and 88150-47-4 are also occured in this study. CODEN: JOAPA6. ISSN: 1225-6110. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The vascular relaxant and antihypertensive effects of newly developed salts of amlodipine - maleate and camsylate - were evaluated on isolated aorta from rats and in spontaneously hypertensive rats, and compared with those of amlodipine besylate, a std. drug. Amlodipine besylate concn.-dependently inhibited Ca2+-induced contraction in depolarized rat aorta(IC50: 4.17 nM), with a very slow onset of action. Amlodipine maleate and amlodipine camsylate also showed vascular relaxant effect with a pattern and a potency similar to those of amlodipine besylate(IC50: 3.62 and 3.28 nM, resp.). Amlodipine besylate produced a dose-dependent and long-lasting( > 10~24 h) antihypertensive effect with a slow onset of action (ED20: 2.31 mg/kg) in spontaneously hypertensive rats. Amlodipine maleate and amlodipine camsylate also exerted antihypertensive effects with a pattern and a potency similar to those of amlodipine besylate (ED20: 2.09 and 2.21 mg/kg, resp.). These results suggest that amlodipine maleate and amlodipine camsylate are not statistically differ with amlodipine besylate in relaxant effect of Ca2+-induced contraction in depolarized rat aorta and in antihypertensive effect in spontaneously antihypertensive rats. .