[3H]AHN 086 acylates peripheral benzodiazepine receptors in the rat pineal gland

FEBS Lett. 1989 Feb 27;244(2):263-7. doi: 10.1016/0014-5793(89)80541-1.


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.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acylation
  • Animals
  • Benzodiazepinones / metabolism*
  • Cattle
  • Chromatography, Gel
  • Electrophoresis, Polyacrylamide Gel
  • Male
  • Molecular Weight
  • Pineal Gland / metabolism*
  • Rats
  • Rats, Inbred Strains
  • Receptors, GABA-A / isolation & purification
  • Receptors, GABA-A / metabolism*
  • Tritium


  • Benzodiazepinones
  • Receptors, GABA-A
  • Tritium
  • AHN 086