Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Effects of a New Selective Phosphodiesterase Type 5 Inhibitor, KJH-1002, on the Relaxation of Rabbit Corpus Cavernosum Tissue

  • Cho, Eun-Young (Bioanalysis & Biotransformation Research Center, Korea Institute of Science and Technology) ;
  • Chung, Sung-Hyun (College of Pharmacy, Kyung Hee University) ;
  • Kim, Joong-Hyup (Biochemicals Research Center Korea Institute of Science and Technology) ;
  • Kim, Dong-Hyun (Bioanalysis & Biotransformation Research Center, Korea Institute of Science and Technology) ;
  • Jin, Cang-Bae (Bioanalysis & Biotransformation Research Center, Korea Institute of Science and Technology)
  • Published : 2003.12.01
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Abstract

The present study examined functional effects of a new selective phosphodiesterase type 5 inhibitor, 1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-thioxo-3-propyl-1H-pyrazolo[ 4,3]pyrimidin-5-yl)phenylsulphonyl]-4-methyl piperazine (KJH-1002), in the isolated rabbit corpus cavernosum (RCC). Relaxing effects of KJH-1002 were also compared with those of sildenafil, which is currently used as an oral therapy for penile erectile dysfunction. In the isolated RCC precontracted with phenylephrine, both KJH-1002 and sildenafil in the concentration range of 1 to 1000 nM, produced a comparable potentiation of the electical field stimulation-induced relaxation in a concentration-dependent manner. In the sodium nitroprusside (SNP)-induced relaxation, the $IC_{50}$/ values, concentrations of SNP required to produce a 50％ relaxation of the phenylephrine-induced contraction, were significantly decreased to the similar extent by treatments with KJH-1002 and sildenafil. The results suggest that a new selective phosphodiesterase type 5 inhibitor, KJH-1002, has an augmentative effect on penile erection comparable to that of sildenafil and can be useful for the treatment of erectile dysfunction.

Keywords

References

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