K. Koike et al., POSSIBLE MECHANISMS OF BETA-ADRENOCEPTOR-MEDIATED RELAXATION INDUCED BY NORADRENALINE IN GUINEA-PIG TAENIA CECUM, European journal of pharmacology, 279(2-3), 1995, pp. 159-163
The mechanisms of the beta-adrenoceptor-mediated relaxation induced by
noradrenaline in guinea pig taenia caecum were investigated. Noradren
aline caused graded relaxation of this preparation. However, the conce
ntration-response curves for noradrenaline were unaffected by proprano
lol (similar to 10(-5) M) or phentolamine (similar to 10(-5) M). The r
esponses to noradrenaline were antagonized in a concentration-dependen
t manner by bupranolol, and Schild plots of the data revealed a pA(2)
value of 5.53. Also, bupranolol antagonized responses to isoprenaline,
and Schild plots of the data revealed the pA(2) value to be 8.53. Nor
adrenaline significantly increased the cyclic AMP level in this prepar
ation. Bupranolol (10(-4) M) significantly decreased the cyclic AMP re
sponse elicited by noradrenaline, whereas propranolol (10(-5) M) produ
ced no effect. These results suggest that the relaxant response to nor
adrenaline in guinea pig taenia caecum is mainly mediated by beta(3)-a
drenoceptors (or atypical beta-adrenoceptors) and that in guinea pig t
aenia caecum noradrenaline behaves as a beta(3)-selective adrenoceptor
agonist.