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.
|Autori:||Martini C; Lucacchini A; Ronca G; Hrelia S; Rossi CA.|
|Titolo:||Isolation of putative benzodiazepine receptors from rat brain membranes by affinity chromatography.|
|Anno del prodotto:||1982|
|Digital Object Identifier (DOI):||10.1111/j.1471-4159.1982.tb10848.x|
|Appare nelle tipologie:||1.1 Articolo in rivista|