Effects of various 2-amino-6-alkyldithiopurines on brain specific [3H]diazepam binding.
Various derivatives of 2-amino-6- methylthiopurine with substituents at the 6-position of purine were tested for their abilities to displace [3H]diazepam binding to rat brain membranes. The potency was dependent on the carbon chain-length in the 6-position of purine. Among the derivatives tested, 2-amino-6-n- pentyldithiopurine had the highest potency, with a Ki value of 0.92 microM.
D000818:Animals; D001921:Brain / Q000378:metabolism*; D002243:Carbolines / Q000378:metabolism; D003975:Diazepam / Q000378:metabolism*; D066298:In Vitro Techniques; D008297:Male; D015122:Mercaptopurine / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology
D002243:Carbolines; D005680:gamma-Aminobutyric Acid; C024915:beta-carboline-3-carboxylic acid ethyl ester; D015122:Mercaptopurine; D003975:Diazepam