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KMID : 0606920030110020013
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Biomolecules & Therapeutics
2003 Volume.11 No. 2 p.13 ~ p.138
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Antihypertensive Effects of Amlodipine Besylate and Its New Salts
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Abstract
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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 standard drug. Amlodipine besylate concentration-dependently inhibited Ca/sup 2＋/-induced contraction in depolarised rat aorta(IC/sub 50/: 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(IC/sub 50/: 3.62 and 3.28 nM, respectively). Amloclipine besylate produced a dose-dependent and long-lasting(>10∼24h) antihypertensive effect with a slow onset of action (ED/sub 20/: 2.31 ㎎/㎏) 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(ED/sub 20/: 2.09 and 2.21 ㎎/㎏, respectively). These results suggest that amlodipine maleate and amlodipine camsylate are not statistically differ with amlodipine besylate in relaxant effect of Ca/sup 2＋/-induced contraction in depolarised rat aorta and in antihypertensive effect in spontaneously antihypertensive rats.
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KEYWORD
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