Journal article

BINDING CHARACTERISTICS OF ( )-, ( /-) AND (-)-[125IODO] CYANOPINDOLOL TO GUINEA-PIG LEFT-VENTRICLE MEMBRANES

D HOYER, G ENGEL, R BERTHOLD

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY | SPRINGER VERLAG | Published : 1982

Abstract

[125Iodo]cyanopindolol [(±)-ICYP], a potent and selective ligand for β-adrenoceptors, exhibited complex biphasic dissociation kinetics. Consequently, in receptor binding studies, the pure (+)- and (-)-enantiomers of ICYP were synthesised and their equilibrium and kinetic binding characteristics were investigated on a membrane preparation of guinea pig left ventricle containing almost only β1-adrenoceptors. All three ligands, i. e. (+)-, (-)- and (±)-ICYP, bind to β-adrenoceptors as assessed by competition experiments with different β-blocking agents; irrespective of the ligand used, the same dissociation constant was found for the competitor. In a first series of saturation binding experimen..

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