title: [Pharmacological characterization of the adrenoceptors in the muscularis mucosae of the guinea-pig esophagus].
abstract: Pharmacological characteristics of the post-junctional adrenoceptors in the muscularis mucosae of the guinea-pig esophagus were examined in vitro. In the presence of propranolol (3 microM), all catecholamines, phenylephrine and methoxamine produced a weak contraction of the isolated muscularis mucosae. The order of potency of the contractile response was adrenaline greater than noradrenaline greater than methoxamine greater than phenylephrine and much weaker isoproterenol, dopamine and clonidine. The contractile responses to noradrenaline (10 microM) and adrenaline (10 microM) were markedly inhibited by phentolamine (3 microM), prazosin (3 microM), indomethacin (1 microM), aspirin (100 microM) and polyphloretin (30 microM), and slightly by yohimbine (3 microM). On the other hand, all catecholamines and terbutaline produced relaxation of the isolated muscularis mucosae which was maximally contracted with carbachol (3 microM) in the presence of phentolamine (10 microM), in a concentration-dependent manner. The order of potency of the inhibitory response was isoproterenol greater than noradrenaline greater than adrenaline and much weaker terbutaline and dopamine. The inhibitory responses to catecholamines were competitively antagonized by three beta blockers, being in the following order of potency as estimated by their pA2 values: propranolol greater than atenolol much greater than butoxamine. The pretreatment of the tissue with indomethacin (1 microM) did not modify the inhibitory responses to catecholamines. These results suggest that the guinea-pig esophageal muscularis mucosae has excitatory alpha 1 adrenoceptors and inhibitory beta 1 adrenoceptors, and the alpha 1, but not beta 1, adrenoceptors may link with the endogenous arachidonic acid cascade.
mesh_terms: D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000818:Animals; D002395:Catecholamines / Q000494:pharmacology; D004947:Esophagus / Q000187:drug effects; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects* / Q000294:innervation; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000502:physiology*; D011943:Receptors, Adrenergic, beta / Q000187:drug effects / Q000502:physiology*; D013566:Sympathomimetics / Q000494:pharmacology
chemical_list: D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D002395:Catecholamines; D011942:Receptors, Adrenergic, alpha; D011943:Receptors, Adrenergic, beta; D013566:Sympathomimetics