Characterization of alpha, beta-methylene ATP binding sites in mouse crude synaptic membranes

Since ATP has been reported to be a potent excitatory transmitter in the mammalian central nervous system (CNS), we studied the neurochemical characters of the binding sites of alpha,beta-methylene ATP, an agonist of P2x receptors, in mouse crude synaptic membranes. ATP and its related compounds inhibited [3H] alpha,beta-methylene ATP binding in a concentration-dependent manner. The potency order in the inhibition of the binding was as follows; alpha,beta-methylene ATP = ADP beta S > ATP gamma S > ATP > or = ADP > beta,gamma-methylene ATP >> UTP > 2-methylthio ATP. And adenosine did not affect the binding. The order was different from those reported in peripheral tissues. And Sr2+, Ca2+, Mg2+, and Cd2+ enhanced the binding. These results suggest that alpha,beta-methylene ATP binding sites in CNS have different characters from those in peripheral tissues.