Autoradiographic differentiation of multiple benzodiazepine receptors by detergent solubilization and pharmacologic specificity

Neurosci Lett. 1983 Aug 19;39(1):37-44. doi: 10.1016/0304-3940(83)90162-3.

Abstract

We have used light microscopic autoradiography to localize differentially Type 1 and 2 benzodiazepine receptors using pharmacologic and detergent treatment techniques. The triazolopyridazine CL218872 has preferential affinity for Type 1 receptors from which it displaces [3H]flunitrazepam selectivity. In biochemical experiments [3H]flunitrazepam binding sites with pharmacologic properties of Type 2 receptors are preferentially solubilized from brain membranes by detergents. We have now treated rat brain slices either with CL218872 or 2% sodium cholate and evaluated the autoradiographic distribution of [3H]flunitrazepam-labeled receptors. Whether calculated from the drug or detergent treated preparations, the relative densities of apparent Type 1 and 2 receptors are the same. Thus differential sensitivity to determine solubilization distinguishes the same two populations of receptors as Type 1 and 2 specific drugs.

Publication types

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

MeSH terms

  • Animals
  • Autoradiography
  • Binding, Competitive
  • Brain / metabolism*
  • Corpus Striatum / metabolism
  • Flunitrazepam / metabolism
  • Neural Pathways / metabolism
  • Pyridazines / metabolism
  • Rats
  • Receptors, Cell Surface / metabolism*
  • Receptors, GABA-A
  • Substantia Nigra / metabolism

Substances

  • Pyridazines
  • Receptors, Cell Surface
  • Receptors, GABA-A
  • Flunitrazepam
  • CL 218872