Isolation of putative benzodiazepine receptors from rat brain membranes by affinity chromatography.
The benzodiazepine receptor from rat brain was solubilised and purified 5200-fold by affinity chromatography. The affinity column contained an immobilized benzodiazepine (delorazepam) and biospecific elution with 6 mM-chlorazepate was achieved. The purified receptor is apparently homogeneous in SDS-polyacrylamide gel electrophoresis. The native protein had a molecular weight of 240,000, and the subunit one of 60,000. The dissociation constant (KD) is 8 nM for [3H]diazepam. A correlation exists between the value of affinity obtained for benzodiazepine derivatives and their known pharmacological effectiveness.
D000818:Animals; D001923:Brain Chemistry; D002846:Chromatography, Affinity / Q000379:methods; D003975:Diazepam / Q000378:metabolism; D008970:Molecular Weight; D051381:Rats; D011955:Receptors, Drug / Q000302:isolation & purification* / Q000378:metabolism; D011963:Receptors, GABA-A
D011955:Receptors, Drug; D011963:Receptors, GABA-A; D003975:Diazepam