Gamma-OH and Sulpiride

patanie at patanie at
Sun Aug 23 04:03:13 EST 1998

Eur J Pharmacol 1998 Apr 10;346(2-3):331-337 

Sulpiride, but not haloperidol, up-regulates
gamma-hydroxybutyrate receptors in vivo and in cultured

Ratomponirina C, Gobaille S, Hode Y, Kemmel V, Maitre M

Laboratoire de Neurobiologie Moleculaire des Interactions Cellulaires,
Strasbourg, France. 

[Medline record in process]

Five days of gamma-hydroxybutyrate (GHB) administration (3 x 500 mg
kg(-1) day(-1) i.p.) to rats
resulted in a significant decrease in the density of GHB receptors
measured in the whole rat brain
without modification of their corresponding affinity. Similar
administration of (-)-sulpiride (2 X 100
mg kg(-1) day(-1) i.p. for 5 days) induces an up-regulation of GHB
receptors without change in
their dissociation constants (Kd). Haloperidol (2 X 2 mg day(-1) i.p.
for 5 days) showed no effect.
Administered chronically via osmotic minipumps directly into the
lateral ventricles, (-)-sulpiride (60
microg day(-1) for 7 days) and GHB (600 microg day(-1) for 7 days)
up-regulated and
down-regulated rat brain GHB receptors, respectively. Finally, in a
mouse hybridoma cell line
(NCB-20 cells) expressing GHB receptors, the treatment of these cells
with 1 mM GHB, 100
microM (-)-sulpiride or 1 mM GABA decreases, increases and induces no
change, respectively, in
the density of GHB receptors after 3 days of treatments. These results
indicate that chronic GHB
treatment modifies the expression of its receptor and that sulpiride
also induces plastic changes in
GHB receptors perhaps via antagonistic properties. 

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