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J Biol Chem, Vol. 273, Issue 27, 16865-16873, July 3, 1998

Cannabinoid Receptor Agonist Efficacy for Stimulating [³⁵S]GTPS Binding to Rat Cerebellar Membranes Correlates with Agonist-induced Decreases in GDP Affinity

From the Department of Physiology and Pharmacology, Center for the Neurobiological Investigation of Drug Abuse, and Center for Investigative Neuroscience, Wake Forest University School of Medicine, Winston-Salem, North Carolina 27157

The relationship between GDP and cannabinoid-stimulated [³⁵S]guanosine-5'-O-(3-thiotriphosphate) ([³⁵S]GTPS) binding was investigated in rat cerebellar membranes. Kinetic analyses showed that [³⁵S]GTPS binding reached steady-state levels and that the association rate was increased by the agonist WIN 55212-2 proportional to the concentration of GDP. Dissociation of [³⁵S]GTPS occurred with two rates (t1/2 = 7 and 170 min), and WIN 55212-2 increased the proportion of sites exhibiting the faster rate. Without GDP, [³⁵S]GTPS bound to membranes with high and low affinity, and WIN 55212-2 had no effect. With 30 µM GDP, [³⁵S]GTPS bound to low and intermediate affinity sites, and WIN 55212-2 induced high affinity [³⁵S]GTPS binding without affecting low affinity sites. GDP competed for high affinity [³⁵S]GTPS binding with high and intermediate affinity in the absence of WIN 55212-2 and with high and low affinity in the presence of WIN 55212-2. Cannabinoid ligands displayed differential abilities to maximally stimulate [³⁵S]GTPS binding in the presence of GDP. Efficacy differences among ligands increased with increasing GDP concentrations. GDP competition curves revealed that agonists induced low affinity GDP K_i values that were proportional to agonist E_max values, indicating that agonist efficacy is determined by displacement of GDP from G-proteins.

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