S-adenosyl-L-homocysteine and 5'-methylthioadenosine inhibit binding of [3H]flunitrazepam to rat brain membranes.
The effect of inhibitors of transmethylation reactions, S-adenosylhomocysteine and 5'-methylthioadenosine, on [3H]flunitrazepam-specific binding to the rat brain membranes has been investigated. Both S-adenosylhomocysteine and 5'-methylthioadenosine are able to inhibit binding with Ki values of 7.9 microM and 15.8 microM respectively. These compounds therefore may be candidate endogenous benzodiazepine-receptor ligands. In light of these and other data possible correlations between phospholipid methylation and gamma-aminobutyric acid (GABA) receptor function are discussed.
D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D003839:Deoxyadenosines / Q000494:pharmacology*; D005445:Flunitrazepam / Q000378:metabolism*; D008745:Methylation; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D012435:S-Adenosylhomocysteine / Q000494:pharmacology*; D013570:Synaptic Membranes / Q000187:drug effects* / Q000378:metabolism; D013872:Thionucleosides / Q000494:pharmacology*; D014316:Tritium
D003839:Deoxyadenosines; D013872:Thionucleosides; D014316:Tritium; D005445:Flunitrazepam; C008500:5'-methylthioadenosine; D012435:S-Adenosylhomocysteine