Posted by SLS on November 10, 2000, at 16:22:50
In reply to Re: reboxetine?, posted by JohnL on November 10, 2000, at 4:30:21
Hi John.
> Many drug trials later I discovered the best cure for my anergic melancholic depressive symptoms was either Amisulpride or Adrafinil, with both together being by far the best. Unfortunately, I'm back into the sexual dysfunction thing and having to struggle to figure out what to do about that.
I am suspicious that dopamine D3 receptor antagonism might be the culprit. Amisulpride is a potent antagonist at this site as well as D2 receptors. Pramipexole (Mirapex) or ropinerole (Requip) might help if this is true.
I guess you have already tried Serzone. I'm not sure it would help very much if the site of action of amisulpride is in the hypothalamus.
If all else fails, you can give sulpiride a try. I have no reason for believing that it would eliminate your complaints, except perhaps that its affinity for D2 and D3 receptors is much lower than that of amisulpride. It is extrememly cheap, and has been around for a long time. It was the first neuroleptic to show a preferential binding to presynaptic autoreceptors. Sulpiride was shown to be effective for depression and dysthymia long before the appearance of amisulpride.
Post a question requesting sex info from sulpiride users.
It is available in quite a few countries. I got my supply from England under the brand name Sulpirex by Squibb. It is also sold under the name of Dogmatil.
- Scott
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: J Pharmacol Exp Ther 2000 Jun;293(3):1063-73S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: II. Functional and behavioral profile compared with GR218,231
and L741,626.Millan MJ, Dekeyne A, Rivet JM, Dubuffet T, Lavielle G, Brocco M
Department of Psychopharmacology, Institut de Recherches Servier, Centre de Recherches de Croissy, Paris, France.
The selective dopamine D(3)-receptor antagonist S33084 dose dependently attenuated induction of hypothermia by 7-hydroxy-2-dipropylaminotetralin (7-OH-DPAT) and PD128,907. S33084 also dose dependently reduced 7-OH-DPAT-induced penile erections (PEs) but had little effect on 7-OH-DPAT-induced yawning and hypophagia, and it did not block contralateral rotation elicited by the preferential D(3) agonist quinpirole in unilateral substantia nigra-lesioned rats. In models of potential antipsychotic activity, S33084 had little effect on conditioned avoidance behavior and the locomotor response to amphetamine and cocaine in rats, and weakly inhibited apomorphine-induced climbing in mice. Moreover, S33084 was inactive in models of potential extrapyramidal activity in rats: induction of catalepsy and prolactin secretion and inhibition of methylphenidate-induced gnawing. Another selective D(3) antagonist, GR218,231, mimicked S33084 in inhibiting 7-OH-DPAT-induced PEs and hypothermia but neither hypophagia nor yawning behavior. Similarly, it was inactive in models of potential antipsychotic and extrapyramidal activity. In distinction to S33084 and GR218,231, the preferential D(2) antagonist L741,626 inhibited all responses elicited by 7-OH-DPAT. Furthermore, it displayed robust activity in models of antipsychotic and, at slightly higher doses, extrapyramidal activity. In summary, S33084 was inactive in models of potential antipsychotic and extrapyramidal activity and failed to modify spontaneous locomotor behavior. Furthermore, it did not affect hypophagia or yawns, but attenuated hypothermia and PEs, elicited by 7-OH-DPAT. This profile was shared by GR218,231, whereas L741,626 was effective in all models. Thus, D(2)-receptors are principally involved in these paradigms, although D(3)-receptors may contribute to induction of hypothermia and PEs. S33084 should comprise a useful tool for further exploration of the pathophysiological significance of D(3)- versus D(2)-receptors.
PMID: 10869411, UI: 20330743
poster:SLS
thread:48528
URL: http://www.dr-bob.org/babble/20001102/msgs/48626.html