Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Antihypertensive Effects of Amlodipine Besylate and Its New Salts

암로디핀의 베실레이트염과 신규 염들의 항고혈압작용 비교평가

  • 이병호 (한국과학연구원 생명의약부) ;
  • 서호원 (한국과학연구원 생명의약부) ;
  • 김맹섭 (한미약품(주)중앙연구소)
  • Published : 2003.06.01
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Abstract

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 $Ca^{2＋}$-induced contraction in depolarised rat aorta($IC_{50}$/: 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($IC_{50}$/: 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$_{20}$: 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(ED$_{20}$: 2.09 and 2.21 mg/kg, respectively). These results suggest that amlodipine maleate and amlodipine camsylate are not statistically differ with amlodipine besylate in relaxant effect of $Ca^{2＋}$-induced contraction in depolarised rat aorta and in antihypertensive effect in spontaneously antihypertensive rats.

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References

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