[Pharmacological analysis of atypical beta-adrenoceptors in the guinea pig gastrointestinal tissue systems].
The purpose of the present study was to characterize the atypical beta-adrenoceptors involved in relaxant responses in guinea pig gastric fundus, duodenum and ileum in functional experiments with catecholamines (isoprenaline, noradrenaline and adrenaline), beta 3-adrenoceptor agonists (BRL37344 and CGP12177A) and a non-selective beta 1-, beta 2- and beta 3-adrenoceptor antagonist bupranolol, and to obtain further evidence to clarify whether there is a tissue difference in atypical beta-adrenoceptors in the guinea pig gastrointestinal tissue systems. The atypical beta-adrenoceptors are present in gastric fundus, duodenum and ileum of guinea pig. In the presence of propranolol (1 microM) or atenolol (100 microM) plus butoxamine (100 microM), bupranolol caused a concentration-dependent rightward shift of the concentration-response curves for catecholamines and beta 3-adrenoceptor agonists. There was not a significant difference of pA2 values for bupranolol against these agonists between gastric fundus, duodenum and ileum of guinea pig. These results suggest that guinea pig gastric fundus, duodenum and ileum relaxation are mediated predominantly by an atypical beta-adrenoceptor population whereas the classical beta 1- or/and beta 2-adrenoceptors play a subordinate function role and that the receptors of three tissues are pharmacological identified by functional approaches. There is not a tissue difference in atypical beta-adrenoceptors in the guinea pig gastrointestinal tissue systems between stomach and ileum.
Horinouchi
T
T
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
Tsujitani
M
M
Koike
K
K
D000318:Adrenergic beta-Agonists / Q000494:pharmacology; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000818:Animals; D002046:Bupranolol / Q000494:pharmacology; D004064:Digestive System / Q000737:chemistry*; D004386:Duodenum / Q000737:chemistry; D004837:Epinephrine / Q000494:pharmacology; D004983:Ethanolamines / Q000494:pharmacology; D005748:Gastric Fundus / Q000737:chemistry; D006168:Guinea Pigs; D007082:Ileum / Q000737:chemistry; D007545:Isoproterenol / Q000494:pharmacology; D008297:Male; D009126:Muscle Relaxation / Q000187:drug effects; D009638:Norepinephrine / Q000494:pharmacology; D011412:Propanolamines / Q000494:pharmacology; D011943:Receptors, Adrenergic, beta / Q000302:isolation & purification*
D000318:Adrenergic beta-Agonists; D000319:Adrenergic beta-Antagonists; D004983:Ethanolamines; D011412:Propanolamines; D011943:Receptors, Adrenergic, beta; C057368:BRL 37344; D002046:Bupranolol; D007545:Isoproterenol; C033394:CGP 12177; D009638:Norepinephrine; D004837:Epinephrine