Amisulpride 99%

Amisulpride 99%

Amisulpride functions primarily as a D2 and D3 receptor antagonist, as well as at 5HT7, with low nanomolar affinity.  Low dose administration demonstrates selective blockade of the pre-synaptic DA autoreceptors. These affinities have demonstrated a high degree of rapid-onset efficacy as an antidepressant.

Research Indications: Antidepressant Research Dopaminergic Research

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Amisulpride functions primarily as a D2 and D3 receptor antagonist with low nanomolar affinity of 2.2nM and 2.4nM respectively.  Low dose administration demonstrates selective blockade of the pre-synaptic autoreceptors.  As well, amisulrpide has high affinity for 5TH7 acting as an potent antagonist at that 5HTR.  These affinities have demonstrated a high degree of rapid-onset efficacy as an antidepressant[1].

To characterize the role of the 5-HT7 receptor in the antidepressant effects of amisulpride, a study prepared 5-HT7 receptor knockout mice. The study found that in two widely used rodent models of depression, the tail suspension test, and the forced swim test, those mice did not exhibit an antidepressant response upon treatment with amisulpride.  These results suggest that 5-HT7 receptor antagonism mediates the antidepressant effects of amisulpride[2].

Interestingly. amisulpride, and the relate sulpride, both bind to the GHB receptor at relevant affinities[3].

Reference Links:

  1. "PRODUCT INFORMATION SOLIAN® TABLETS and SOLUTION" (PDF). TGA eBusiness Services. Sanofi-Aventis Australia Pty Ltd. 9 September 2013. Retrieved 17 October 2013.
  2. Abbas, AI; Hedlund, PB; Huang, XP; Tran, TB; Meltzer, HY; Roth, BL (2009). "Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo"Psychopharmacology 205 (1): 119–128. doi:10.1007/s00213-009-1521-8PMC 2821721PMID 19337725.
  3. Maitre, M.; Ratomponirina, C.; Gobaille, S.; Hodé, Y.; Hechler, V. (Apr 1994). "Displacement of [3H] gamma-hydroxybutyrate binding by benzamide neuroleptics and prochlorperazine but not by other antipsychotics". European Journal of Pharmacology 256 (2): 211–214. doi:10.1016/0014-2999(94)90248-8.PMID 7914168.

USAGE: For Research Use Only! Not For Use in Humans.

ARTICLE:

Amisulpride : A forgotten "Old-School" AntiPsychotic with A Superior Anti-Depressant Profile & Unique Mechanism of Action (Little to no side-effects)

Amisulpride certainly doesn't carry the wide array of pharmacological actions that most "familiar" or "Atypical Antipsychotics" do, but that doesn't make it any less potent(1)

AMISULPRIDE HAS FAR LESS SIDE-EFFECTS
One distinguishable trait of amisulpride is that lower doses seem to only, or mostly block the dopamine D2S (autoreceptors) (2)  - which leads to an actual enhancement in dopamine release(3). Most of the usual antipsychotics we hear about, e.g risperidone, thorazine and haldol - all have very potent dual action dopamine receptor blockade(4). This leads to many more side-effects, including incidences of depression and high rates of drug-induced tardive dyskinesia(5).

Additionally, most anti-psychotic drugs have extremely potent alpha-1-adrenergic receptor blockade(6) (7)amisulpride lacks this property, as well as the usual anti histamine property of anti-psychotics (8) - which means AmiSulpride is very unlikely to cause any form of sedation(9).

Usually, the anti-histamine properties of other anti-psychotic drugs combined with the alpha-1-blockade - acts as a one-two punch in knocking the patient out cold....frequently we hear about some of the affected even drooling on themselves or just completely incoherent and lethargic the following day(10)!

While some medical professionals consider this a benefit in hostile or unpredictable patients, I would find it much less than ideal for someone who wants to maintain somewhat of a normal life , not incapacitated but with symptoms controlled(11).

Besides lack of side-effects, or at least lack of sedation - amisulpride has one very notable effect that sets it apart from other drugs in its class - it's anti-depressant effects are VERY FAST ACTING, very potent - and generally yield little to no negative endocrine effects(12).

The mechanism of action is totally unique, amisulpride binds to the serotonin 5-HT(7) with 11.5 nanomolar (ki/nm) affinity - this includes in human subjects(14).
It antagonizes the action of serotonin at this receptor - resulting in an anti-depressant effect that can not only augment other anti-depressants - but can be much more effective alone than many anti-depressants(15).

The additional benefits of 5-HT(7) antagonism are that it will reduce overstimulation and anxiety - as well as treat depression - and lower cortisol levels as well(16).

Because many depressed patients exhibit HPAA (hypothalamic-pituitary-adrenal-axis) dysfunction - and often have elevated cortisol - this unique mechanism of action may benefit the hormonal balance of depressed patients..(17) unlike SSRI's which tend to increase stress hormones (18) and oppose other beneficial neurotransmitters such as GABA, dopamine and others(19)!

Thus, in summary...

Amisulpride has the following benefits / advantages over other drugs aiming to do the same.
  • A cortisol reduction, instead of increase.
  • Enhances dopamine at lower doses.
  • Little to no sedation, drowsiness, dyskinesia, tremors , punding or other disturbing side-effects.
  • Doesn't interfere with cognitive function or vigilance.
  • Treats depression quickly , and effectively.
  • May improve anxiety symptoms as well.

USAGE: For Research Use Only! Not For Use in Humans.