Pharmacological characterization of the beta-adrenoceptor that mediates the relaxant response to noradrenaline in guinea-pig tracheal smooth muscle

Naunyn-Schmiedeberg's Archives of Pharmacology
Y TanakaK Koike

Abstract

Pharmacological characteristics of beta-adrenoceptors (beta-ARs) mediating noradrenaline-induced relaxation were investigated in guinea-pig tracheal smooth muscle. The inhibitory effects of several types of beta-AR antagonists on noradrenaline-induced relaxation against histamine contraction were scrutinized with Schild plot analysis. The concentration-response curve for noradrenaline obtained in the absence of phentolamine and uptake inhibitors was competitively antagonized by all of the beta-AR antagonists used in this study (propranolol, bupranolol, atenolol, butoxamine and ICI-118,551). However, their pA2 values were markedly less than the expected values for beta1-AR and beta2-AR. On the other hand, pA2 values of ICI-118,551 (6.85) determined in the presence of phentolamine suggested a contribution of a beta1 -AR rather than beta2 -AR. In the presence of phentolamine and uptake inhibitors (desipramine and deoxycorticosterone), the Schild plot for atenolol was a better fit, with two distinct straight lines. The pA2 values of atenolol provided by the regression were: approximately 7.0, which corresponds to the expected beta1-AR value, and approximately 6.5, which was 3 times less than the expected value for beta1 -AR, and th...Continue Reading

References

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Citations

Jun 13, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Martin C Michel, Sergio Parra
Oct 4, 2011·Journal of Receptor and Signal Transduction Research·Y TanakaY Kasuya
Mar 16, 2018·Journal of Smooth Muscle Research = Nihon Heikatsukin Gakkai Kikanshi·Daisuke ChinoY Tanaka
Feb 18, 2011·British Journal of Pharmacology·J Daniel HothersallJames R Baker

Related Concepts

ICI 118551, hydrochloride
1-(2-((3-carbamoyl-4-hydroxy)phenoxy)ethylamino)-3-(4-(1-methyl-4-trifluoromethyl-2-imidazoylyl)phenoxy)-2-propanol methanesulfonate
Adrenergic alpha-Antagonists
Adrenergic beta-Antagonists
Sultanol
Tenormin
Betadrenol
Butoxamine Hydrochloride
ratio-Desipramine
Deoxycorticosterone

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