Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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General Pharmacology of DA-5018, a New Capsaicin Derivative

새로운 캅사이신유도체 DA-5018외 일반약리작용

  • 김순희 (동아제약주식회사 연구소) ;
  • 손문호 (동아제약주식회사 연구소) ;
  • 신명수 (동아제약주식회사 연구소) ;
  • 김희기 (동아제약주식회사 연구소) ;
  • 배은주 (동아제약주식회사 연구소) ;
  • 차봉진 (동아제약주식회사 연구소) ;
  • 김원배 (동아제약주식회사 연구소) ;
  • 양중의 (동아제약주식회사 연구소)
  • Published : 1997.03.01
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Abstract

DA-5018(N-(3-(3, 4-dimethylphenyl)propyl)-4-(2-aminoethoxy)-3-methoxyphenylacetamide) is a new capsaicin derivative under development as topical analgesic agent. The general pharmacological properties of DA-5018 on central nervous, cardiovascular, gastrointestinal and other organ systems were studied in experimental animals. DA-5018 cream (0.3%) had no effects on behavior, hexobarbital-induced sleeping time, body temperature, spontaneous activity, blood pressure, heart rate, intestinal charcoal propulsion, urine volume and electrolyte excretion even at a high dose of 2000 mg/kg in rats. In addition, DA-5Ol8 cream had little skin irritation compared to Zostrix-HP (capsaicin, 0.075%) cream in rabbits. In isolated guinea pig tissue studies, DA-5018 increased the contractility of trachea and ileum and also increased sinus rate of atrium in a range of 10^{-8}-10^{-5}$$ M, but its efficacy as a agonist was weak. These results suggest that DA-5018 cream might be used topically without serious side effects.

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