Inhibitors of peripheral-type benzodiazepine receptors present in human urine and plasma ultrafiltrates.
Several endogenous substances that inhibit central-type benzodiazepine (BZD) receptor binding have recently been identified. We have found that ultrafiltrates of human uremic plasma, normal plasma, and urine contain competitive inhibitors of peripheral-type benzodiazepine receptors. Using urine as source, we have partially purified a peripheral-type BZD receptor inhibitor(s) by adsorption to and selective elution from small octadecyl-silane (Sep-pak) columns and thin layer chromatography. The inhibitor has a 125-fold greater affinity for peripheral-type than central-type BZD receptors and has been purified 8000-fold from urine.
D000327:Adsorption; D014151:Anti-Anxiety Agents / Q000037:antagonists & inhibitors*; D001569:Benzodiazepines; D001667:Binding, Competitive; D002855:Chromatography, Thin Layer; D006801:Humans; D007676:Kidney Failure, Chronic / Q000378:metabolism; D008024:Ligands; D011956:Receptors, Cell Surface / Q000187:drug effects*; D011963:Receptors, GABA-A; D014462:Ultrafiltration; D014511:Uremia / Q000378:metabolism
D014151:Anti-Anxiety Agents; D008024:Ligands; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; D001569:Benzodiazepines