Effect of synthetic purines and purine nucleosides on [3H]diazepam binding in brain.

S C Sung, M Saneyoshi

European journal of pharmacology 1982 Jul 16

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We have compared fifteen synthetic purines and purine nucleosides on their ability to displace [3H]diazepam binding to rat brain membranes. Among these analogs, 6-methylthioguanine was found to be most potent, inhibiting competitively the specific binding of [3H]diazepam with a Ki value of 16 micro M. At a concentration of 50 micro M, 6-methyl-thioguanine increased tha apparent Kd of specific diazepam binding from 4.3 nM to 13.3 nM without affecting the Bmax, nor had it any effect on the non-specific binding. Binding with membrane preparations from developing rat brain was slightly less sensitive to 6-methylthioguanine inhibition than that with membranes prepared from mature brain.

Citation

S C Sung, M Saneyoshi. Effect of synthetic purines and purine nucleosides on [3H]diazepam binding in brain. European journal of pharmacology. 1982 Jul 16;81(3):505-8