The GHB antagonist NCS-382

Claude de Contrecoeur cyrano at
Wed Apr 16 08:31:48 EST 1997

Physiol Behav 58 (3): 587-590 (1995)

Blockade of the discriminative stimulus effects of
acid (GHB) by the GHB receptor antagonist NCS-382.

Colombo G, Agabio R, Bourguignon J, Fadda F, Lobina C, Maitre M, Reali
Schmitt M, Gessa GL

Dipartimento di Neuroscienze "Bernard B. Brodie", Universita di

The present study was designed to assess the ability of the newly
synthetized, selective gamma-hydroxybutyric acid (GHB) receptor
NCS-382, in blocking the discriminative stimulus effects of GHB in a
T-maze, food-reinforced drug discrimination procedure. Two groups of
were trained to run the left arm of the maze 30 min after the i.g.
administration of either 300 or 700 mg/kg GHB and the right arm after
water. Once discrimination was acquired, combination of different
doses of
NCS-382 (0, 12.5, 25.0 and 50.0 mg/kg, IP) and GHB training doses were
tested for blockade of GHB discrimination. NCS-382 dose-dependently
GHB-appropriate responding in both the 300 and 700 mg/kg GHB rat
The results of the present study indicate that the discriminative
properties of GHB are mediated via stimulation of GHB receptors.

MeSH Terms:

   * Animal
   * Anticonvulsants/pharmacology*
   * Appetitive Behavior/drug effects*
   * Benzocycloheptenes/pharmacology*
   * Brain/drug effects
   * Discrimination Learning/drug effects*
   * Dose-Response Relationship, Drug
   * Male
   * Maze Learning/drug effects*
   * Neurons/drug effects
   * Rats
   * Receptors, Cell Surface/antagonists & inhibitors*
   * Sodium Oxybate/pharmacology
   * Sodium Oxybate/antagonists & inhibitors*
   * Support, Non-U.S. Gov't


   * Sodium Oxybate
   * NCS 382
   * 4-hydroxybutyric acid receptor
   * Receptors, Cell Surface
   * Benzocycloheptenes
   * Anticonvulsants

PMID: 8587968, MUID: 96172731


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