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The existence of a specific synthesizing enzyme for gamma-hydroxybutyric acid in rat brain has recently been reported. Here, for the first time, we demonstrate the presence of a high affinity, apparently specific binding site for this compound in the same tissue. This binding does not require Na+ and takes place optimally at pH 5.5. The bound(More)
The behavioral effects of specific cAMP phosphodiesterase inhibitors (PDE-I) such as rolipram and structurally related compounds were investigated in mice. Selected PDE-I induced a potent dose-dependent decrease in locomotion and in rearing of mice confronted with a free exploratory procedure, these effects being considered as a behavioral sedation.(More)
CGS 15943A is the first reported nonxanthine adenosine antagonist and it shows high affinity towards A1 and A2 receptors. The present data show that CGS 15943A increased in a dose-dependent manner locomotor activity of mice confronted with a free exploratory test without markedly modifying rears or, at low or medium doses, novelty seeking responses. In the(More)
BACKGROUND AND PURPOSE Opiates remain the most effective compounds for alleviating severe pain across a wide range of conditions. However, their use is associated with significant side effects. Neuropeptide FF (NPFF) receptors have been implicated in several opiate-induced neuroadaptive changes including the development of tolerance. In this study, we(More)
NCS-382 possesses antagonistic properties at gamma-hydroxybutyrate receptor sites. Its effect on the sedative/cataleptic behaviour observed in rats after gamma-hydroxybutyrate administration was investigated. NCS-382 diminished, in a dose-dependent manner, the sedative and/or cataleptic effects of gamma-hydroxybutyrate, as revealed by a variety of(More)
Previous data have shown that HEPES, a taurine structural analog, inhibits the uptake of taurine by cultured cells differently, depending on its addition either to the culture medium or to the Krebs-Ringer buffer used for cell incubation during taurine uptake measurements (Lleu and Rebel, J Neurosci Res 23: 78-86, 1989). An extensive study of the effect of(More)
Administration of gamma-hydroxybutyrate (GHB) to animals induces electroencephalographic and behavioral changes that resemble petit-mal seizures. Furthermore, these GHB-induced electroencephalogram-behavioral changes can be blocked by anticonvulsant drugs, which are specific in their action against petit-mal seizures. These effects of GHB on(More)
Gamma-hydroxybutyrate (GHB) at low doses (5-10 mg/kg i.p.) increased and at high doses (160-320 mg/kg i.p.) decreased the spontaneous firing rate of prefrontal cortex (PFC) neurons recorded in urethane-anesthetized rats. Only excitations were blocked by NCS-382, a specific GHB receptor antagonist; this suggests that the excitatory effect of low doses of GHB(More)
The effects of derivatives of gamma-hydroxybutyrate (GHB) and gamma-butyrolactone were examined in Wistar rats from a strain in which spontaneous spike-and-wave discharges can be recorded electroencephalographically. For each compound, the effects were compared to those obtained in rats from a strain without spontaneous seizures. Administration of GHB(More)
gamma-Hydroxybutyrate (GHB) is a compared with numerous neuropharmacological properties. The discovery of its biosynthetic system, together with its endogenous repartition, have prompted its possible implication in neurotransmission. The role is also supported by the existence, reported here, of a high-affinity uptake system for GHB (Km = 46.4 microM) in(More)