Assay Method Information

Assay Name:  Binding Assay
Description:  Binding to the rat alpha-1 adrenergic receptor in rat brain membranes was determined by displacement of 3[H]-prazosin (P. Greengrass and R. Bremner; Binding characteristics of 3H-prazosin to rat brain a-adrenergic receptors. Eur. J. Pharmacol. 1979, 55: 323-326). Compounds were incubated at 0.3 or 3 μM final concentration, in duplicate, and the amount of displaced 3[H]-prazosin determined by liquid scintillation spectroscopy.Binding IC50 values were determined from displacement curves (four-six concentrations, each concentration in duplicate) fit by a non-linear, least squares, regression analysis using MathIQ (ID Business Solutions Ltd., UK). The binding Ki's were determined from the IC50 according to the method of Cheng and Prusoff (Y. Cheng and W. H. Prusoff, Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 percent inhibition (IC50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22: 3099-3108).
Affinity data for this assay
 

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