Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Antihypertensive Effect of Amlodipine Adipate, a Novel Salt of Amlodipine, in Hypertensive Rat Models

  • Lee, Byung-Ho (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Seo, Ho-Won (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Chae, Myeong-Yun (R&D Center of Pharmaceuticals, CJ Corp.) ;
  • Yeon, Kyu-Jeong (R&D Center of Pharmaceuticals, CJ Corp.)
  • Published : 2004.03.01
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Abstract

The vascular relaxant effect of amlodipine adipate, a new salt of amlodipine, was evaluate in isolated rat aorta, and compared with that of amlodipine besylate. Furthermore, antihypertensive effects were measured in hypertensive rat models, such as spontaneously hypertensive rats (SHR) and rena1 hypertensive rats (RHR). Amlodipine adipate concentration-dependently inhibited $Ca^{2+}$-induced contraction of rat aorta with a very slow onset of action (reached its maximum at 3.5 h;$IC_{50}$: 3.76 nM), having a pattern and a potency similar to those of amlodipine besylate ($IC_{50}$: 4.01 nM). In SHR and RHR, orally administered amlodipine adipate produced a dosedependent and long-lasting (>10-24 h) antihypertensive effect ($ED_{20}$: 2.48 and 1.57 mg/kg, respectively), with a pattern and a potency similar to those of amlodipine besylate ($ED_{20}$: 2.50 and 1.99 mg/kg in SHR and RHR, respectively). These results suggest that amlodipine adipate is a potent and long-lasting antihypertensive agent and that its antihypertensive effect is not significantly different to that of amlodipine besylate.

Keywords

References

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