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Antihypertensive Effects of Enantiomers of Amlodipine Camsylate, a Novel Salt of Amlodipine
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  • Antihypertensive Effects of Enantiomers of Amlodipine Camsylate, a Novel Salt of Amlodipine
  • Antihypertensive Effects of Enantiomers of Amlodipine Camsylate, a Novel Salt of Amlodipine
저자명
Oh. Kwang-Seok,Kim. Maeng-Sup,Lee. Byung-Ho
간행물명
The journal of applied pharmacology : the official journal of the Korean Society of Applied Pharmacology
권/호정보
2007년|15권 1호|pp.40-45 (6 pages)
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한국응용약물학회
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

The vascular relaxant effects on isolated rat aorta of amlodipine camsylates (S-, R-enantiomer, and R/S-racemate), were evaluated and compared with that of S-amlodipine besylate. Furthermore, antihypertensive effects were measured in spontaneously hypertensive rat (SHR). The S-amlodipine camsylate concentration-dependently inhibited $Ca^{2+}$-induced contraction of rat aorta with a very slow onset of action (reached its maximum at 3.5h; $ED_{50}:;1.50;{pm};0.24$ nM), having a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{50}:;3.36;{pm};0.91;nM)$ and similar to those of S-amlodipine besylate $(ED_{50}:;1.44;{pm};0.14;nM)$, whereas the R-amlodipine camsylate has 590-fold lower vasorelaxant activity $(ED_{50}:;886.4;{pm};49.7;nM)$. In SHR, orally administered S-amlodipine camsylate produced a dose-dependent and long-lasting (>>10 h) antihypertensive effect $(ED_{20}:;0.89;mg/kg)$, with a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{20}:;1.82;mg/kg)$ and similar to those of S-amlodipine besylate $(ED_{20}:;0.71;mg/kg)$. In contrast, the R-amlodipine camsylate has no effect even-though administrated high concentration 10 mg/kg. These results suggest that S-amlodipine camsylate has the potency and long-lasting antihypertensive activity as single enantiomer drug, and its antihypertensive effect is not significantly different to that of S-amlodipine besylate.