Anti-sedative and anti-cataleptic properties of NCS-382, a gamma-hydroxybutyrate receptor antagonist.
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 sensorimotor tests. These results indicate that the well-known sedative/anaesthetic effects induced by gamma-hydroxybutyrate administration are provoked via stimulation of a specific class(es) of gamma-hydroxybutyrate receptors which exist in the rat brain and which could mediate a local stimulation of opiate synthesis and release.
Schmidt
C
C
Centre de Neurochimie, CNRS, Strasbourg, France.
Gobaille
S
S
Hechler
V
V
Schmitt
M
M
Bourguignon
J J
JJ
Maitre
M
M
D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001567:Benzocycloheptenes / Q000494:pharmacology*; D002375:Catalepsy / Q000139:chemically induced / Q000517:prevention & control*; D004305:Dose-Response Relationship, Drug; D006220:Haloperidol / Q000494:pharmacology; D006993:Hypnotics and Sedatives / Q000037:antagonists & inhibitors*; D008297:Male; D011597:Psychomotor Performance / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D012978:Sodium Oxybate / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D013469:Sulpiride / Q000494:pharmacology; D013550:Swimming
D000927:Anticonvulsants; D001567:Benzocycloheptenes; D006993:Hypnotics and Sedatives; C066471:NCS 382; D012978:Sodium Oxybate; D013469:Sulpiride; D006220:Haloperidol