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  • Title: [3H]AHN 086 acylates peripheral benzodiazepine receptors in the rat pineal gland.
    Author: McCabe RT, Schoenheimer JA, Skolnick P, Newman AH, Rice KC, Reig JA, Klein DC.
    Journal: FEBS Lett; 1989 Feb 27; 244(2):263-7. PubMed ID: 2537753.
    Abstract:
    AHN 086, an isothiocyanato derivative of Ro 5-4864 (4'-chlorodiazepam), inhibits radioligand binding to peripheral benzodiazepine receptors with characteristics of an irreversible (acylating) ligand. We now report that [3H]AHN 086 labels a approximately 30 kDa protein in the rat pineal gland determined by both SDS-polyacrylamide gel electrophoresis and gel filtration high-performance liquid chromatography of digitonin-solubilized membranes. Specific incorporation of [3H]AHN 086 into this protein was inhibited by preincubating membranes with excess AHN 086. Moreover, significant specific binding of [3H]AHN 086 was not observed in either bovine pineal gland (which does not possess high-affinity binding sites for Ro 5-4864) or ovalbumin. These findings suggest that the approximately 30 kDa protein labeled by [3H]AHN 086 in rat pineal gland is associated with peripheral benzodiazepine receptors in this tissue.
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