General pharmacology · 1995
Effect of bupranolol on CGP 12177-induced relaxation and cAMP accumulation in the guinea pig taenia caecum.
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Koike K, Horinouchi T, Takayanagi I
Аннотация
1. The effect of bupranolol on CGP 12177-induced relaxation and cAMP accumulation in the guinea pig taenia caecum was examined. 2. The relaxant response to CGP 12177 was unaffected by propranolol (approximately 10(-6) M), whereas that to CGP 12177 was antagonized in a concentration-dependent manner by bupranolol; Schild plot of the data revealed the pA2 value of 5.61. 3. CGP 12177 significantly increased cyclic AMP level in this preparation. Bupranolol (10(-4) M) significantly decreased the cyclic AMP level that was elicited by CGP 12177, whereas propranolol (10(-5) M) produced no effect. 4. These results suggest that bupranolol appears to be an efficient beta3-antagonist in the guinea pig taenia caecum and confirm that the response to CGP 12177 is mediated by beta3-adrenoceptors.