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Different apparent modes of inhibition of alpha2A-adrenoceptor by alpha2-adrenoceptor antagonists.

Abstract：

:The inhibition of alpha2A-adrenoceptor-mediated Ca2+ elevation by alpha2-adrenoceptor antagonists was measured in HEL human erythroleukemia cells. The antagonists could be divided in two classes: those that displayed surmountable inhibition (right-shift of the agonist dose-response curve), and those that displayed different degrees of insurmountable inhibition (depression of the maximum signal and a possible right-shift of the agonist dose-response curve). The degree of surmountability of the inhibition correlated well with the measured antagonist dissociation rates, suggesting that the hypothesis of the antagonist dissociation rate governing the mode of inhibition of fast responses, holds true. HEL cells thus provide a useful model system for the investigation of physiological consequences of different dissociation rates. Also, the dissociation rates of antagonists not available in radiolabelled form can be predicted from the functional data. The data stresses the importance of measurement of kinetic parameters of the drug-receptor interaction in addition to the equilibrium binding constants.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Kukkonen JP,Huifang G,Jansson CC,Wurster S,Cockcroft V,Savola JM,Akerman KE

doi

10.1016/s0014-2999(97)01180-1

subject

Has Abstract

pub_date

1997-09-17 00:00:00

pages

99-105

issue

1

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(97)01180-1

journal_volume

335

pub_type

杂志文章

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