Regulation of [3H]forskolin binding to human platelet membranes by GppNHp, NaF, and prostaglandin E1.

Displaceable binding of [3H]forskolin to human platelet membranes can be detected in the presence of magnesium. There is an increase in the number of [3H]forskolin binding sites when membranes are incubated with GppNHp or NaF in the presence of magnesium. Prostaglandin E1, which stimulates human platelet adenylate cyclase, does not affect the binding of [3H]forskolin in the absence of GppNHp. However, the dose-response curve for the GppNHp-dependent increase in [3H]forskolin binding sites is shifted to lower concentrations in the presence of prostaglandin E1. Prostaglandin E1 potentiates the effect of GppNHp on [3H]forskolin binding most likely by facilitating the binding of the guanine nucleotide at the stimulatory quanine nucleotide regulatory protein of adenylate cyclase.