The effect of GTP on benzodiazepine receptors

Eur J Pharmacol. 1982 Jan 8;77(1):57-9. doi: 10.1016/0014-2999(82)90536-2.

Abstract

GTP decreases the specific binding of [3H]flunitrazepam to cerebral cortical membrane sites. Scatchard analysis data show that GTP does not alter the maximum binding sites (Bmax), but increases the dissociation constant (KD) for [3H]flunitrazepam. GTP also inhibits the specific binding of the benzodiazepine antagonist [3H]CGS-8216. The specific binding of [3H]CGS-8216 displaceable by clonazepam is inhibited to a greater extent by GTP than that displaceable by the benzodiazepine antagonists, CGS-8216 or beta-CCE.

Publication types

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

MeSH terms

  • Animals
  • Benzodiazepines / antagonists & inhibitors
  • Binding, Competitive / drug effects
  • Brain / metabolism*
  • Cattle
  • Cell Membrane / metabolism
  • Flunitrazepam / metabolism
  • Guanosine Triphosphate / pharmacology*
  • In Vitro Techniques
  • Pyrazoles / metabolism
  • Receptors, Drug / drug effects*
  • Receptors, Drug / metabolism
  • Receptors, GABA-A

Substances

  • Pyrazoles
  • Receptors, Drug
  • Receptors, GABA-A
  • Benzodiazepines
  • Flunitrazepam
  • 2-phenylpyrazolo(4,3-c)quinolin-3(5H)-one
  • Guanosine Triphosphate