European Journal of Pharmacology 1982-07-16

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

S C Sung, M Saneyoshi

Index: Eur. J. Pharmacol. 81(3) , 505-8, (1982)

Full Text: HTML

Abstract

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.

Related Compounds

  • Purine, 2-amino-6-...

Related Articles:

Liquid Chromatography with Amperometric Detection at a Silver Based Detector for the Determination of Thiocompounds: Application to the Assay of Thiopurine Antimetabolites in Urine.

2015-07-07

[Anal. Chem. 87 , 6730-5, (2015)]

The syntheses and properties of tricyclic pyrrolo[2,3-d]pyrimidine analogues of S6-methylthioguanine and O6-methylguanine.

2006-05-07

[Org. Biomol. Chem. 4(9) , 1723-9, (2006)]

Reference intervals for thiopurine S-methyltransferase activity in red blood cells using 6-thioguanine as substrate and rapid non-extraction liquid chromatography.

2004-07-01

[Ann. Clin. Biochem. 41(Pt 4) , 303-8, (2004)]

Effects of various 2-amino-6-alkyldithiopurines on brain specific [3H]diazepam binding.

1984-06-01

[Biochem. Pharmacol. 33 , 1737-1739, (1984)]

Role of postreplicative DNA mismatch repair in the cytotoxic action of thioguanine.

1996-08-23

[Science 273(5278) , 1109-11, (1996)]

More Articles...