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sulpiride upregulates GHB receptors

MeDieViL

MeDieViL

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Feb 11, 2007
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Eur J Pharmacol. 1998 Apr 10;346(2-3):331-7.
Sulpiride, but not haloperidol, up-regulates gamma-hydroxybutyrate receptors in vivo and in cultured cells.

Ratomponirina C, Gobaille S, Hodé Y, Kemmel V, Maitre M. Laboratoire de Neurobiologie Moléculaire des Interactions Cellulaires, UPR 416 CNRS, Strasbourg, France.

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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sulpiride just as amisulpride can be used as an antidepressant in low doses (as it only blocks the presynaptic dopamine receptors, thus increasing the ammount of dopamin, those 2 are also reported to be helpfull with social anxiety), might be a good option to treat GHB addiction or the lasting damage it caused
 
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MeDieViL said:
sulpiride just as amisulpride can be used as an antidepressant in low doses (as it only blocks the presynaptic dopamine receptors, thus increasing the ammount of dopamin, those 2 are also reported to be helpfull with social anxiety), might be a good option to treat GHB addiction or the lasting damage it caused
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Sulpiride is an interesting antidepressant in low doses.
 
so that means that sulpiride/amisulpride selectively antagonize d2-autoreceptors, at least in moderate doses of ~100mg, to boost dopamine-release (without blockade of postsynaptic dopamine-receptors like common neuroleptics) and therefore should be lifting mood and generally be reinforcing.

i'm nterested in this especially as i do have some sulpiride lying around for 5 years now but never ate them :)
 
have you got a tolerance for G? would be interesting to see if it lowers your G tolerance, be carefull tough as making those receptors more sensitive could increase the risk of getting an overdose
 
That paper is shit house. GHB binds to lots of things, lots of things that have nothing to do with its psychological effect. Hard to tell from that paper how much what looking at is GABA-B receptor and what isn't.
 
I wouldn't bother with it, there are better ways to boost dopamine. This is an antipsychotic, I dont think it's going todo much boosting
 
I wouldn't bother with it, there are better ways to boost dopamine. This is an antipsychotic, I dont think it's going todo much boosting
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Low doses preferentially stimulate the autoreceptors and are dopaminergic. It has helped some people as an antidepressant in this regard.
 
(zonk) said:
I wouldn't bother with it, there are better ways to boost dopamine. This is an antipsychotic, I dont think it's going todo much boosting
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It's an antidepressant in low doses.
 
Some time ago I was suffering from real bad, disabeling depression. Tried all the standard medications such as SSRI and mirtazapine, but nothing helped. Then started low-dose amisulpride (50mg in the morning), and within a few days the depression was gone, without any side effects. Now taking still 100mg amisulpride in the morning to stabilize my mood and fight my dysthymia. A friend of mine made similar positive experiences with amisulpride. For some people it is a real miracle cure and is highly recommended for treatment resistant depression and particularly dysthymia.
 
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