International journal of urology : official journal of the Japanese Urological Association · 2008
Effects of a novel beta(3)-adrenoceptor agonist, AJ-9677, on relaxation of the detrusor muscle: an in vitro study.
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Otsuka Atsushi, Shinbo Hitoshi, Hasebe Ko, Matsumoto Rikiya, Ozono Seiichiro
Аннотация
OBJECTIVES: To examine the relaxant effects of AJ-9677, a novel beta(3)-adrenoceptor agonist, on the isolated rat, monkey and human detrusor muscle.
METHODS: The isolated detrusor strips of rats, monkeys and humans were mounted in organ baths containing Krebs solution. By the cumulative addition of beta-adrenoceptor agonists (isoproterenol, AJ-9677, CL 316,243 and salbutamol in rats; isoproterenol, AJ-9677 and CL 316,243 in monkeys and humans), concentration-relaxation curves were obtained. The maximal relaxation responses and pEC(50) values were calculated. In rats, concentration-relaxation curves to isoproterenol and AJ-9677 were obtained in the presence and absence of propranolol or SR 59230A.
RESULTS: Isoproterenol, AJ-9677, CL 316,243 and salbutamol induced concentration-dependent relaxation in rats. The rank order of their relaxing potency in the rat detrusor muscle was AJ-9677 > isoproterenol > CL 316,243 > salbutamol. Isoproterenol and AJ-9677 also produced a concentration-dependent relaxation with high potency in monkeys and humans, whilst CL 316,243 had low relaxing potency. According to the antagonist studies in rats, propranolol and SR 59230A caused a rightward shift of the concentration-relaxation curves to isoproterenol or AJ-9677, respectively.
CONCLUSIONS: AJ-9677 has a high relaxant potency on the rat, monkey and human detrusor smooth muscle, and it may have the potential to treat overactive bladder.
METHODS: The isolated detrusor strips of rats, monkeys and humans were mounted in organ baths containing Krebs solution. By the cumulative addition of beta-adrenoceptor agonists (isoproterenol, AJ-9677, CL 316,243 and salbutamol in rats; isoproterenol, AJ-9677 and CL 316,243 in monkeys and humans), concentration-relaxation curves were obtained. The maximal relaxation responses and pEC(50) values were calculated. In rats, concentration-relaxation curves to isoproterenol and AJ-9677 were obtained in the presence and absence of propranolol or SR 59230A.
RESULTS: Isoproterenol, AJ-9677, CL 316,243 and salbutamol induced concentration-dependent relaxation in rats. The rank order of their relaxing potency in the rat detrusor muscle was AJ-9677 > isoproterenol > CL 316,243 > salbutamol. Isoproterenol and AJ-9677 also produced a concentration-dependent relaxation with high potency in monkeys and humans, whilst CL 316,243 had low relaxing potency. According to the antagonist studies in rats, propranolol and SR 59230A caused a rightward shift of the concentration-relaxation curves to isoproterenol or AJ-9677, respectively.
CONCLUSIONS: AJ-9677 has a high relaxant potency on the rat, monkey and human detrusor smooth muscle, and it may have the potential to treat overactive bladder.