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Amisulpride is believed to work by blocking, or antagonizing, the dopamine D 2 receptor, reducing its signalling. The effectiveness of amisulpride in treating dysthymia and the negative symptoms of schizophrenia is believed to stem from its blockade of the presynaptic dopamine D 2 and D 3 autoreceptors.
A dosage of 50 mg/day N-methylamisulpride has been found to achieve 60 to 80% occupancy of the dopamine D 2 receptor, whereas 300 to 400 mg/day amisulpride achieved around 70% occupancy and doses of 630 to 910 mg/day amisulpride achieved 70 to 80% occupancy of the receptor. [4] [6] Amisulpride has been associated with QT prolongation.
Dopamine receptor flow chart. Dopamine receptors are all G protein–coupled receptors, and are divided into two classes based on which G-protein they are coupled to. [1] The D 1-like class of dopamine receptors is coupled to Gα s/olf and stimulates adenylate cyclase production, whereas the D 2-like class is coupled to Gα i/o and thus inhibits adenylate cyclase production.
SEP-4199, also known as non-racemic amisulpride, is a non-racemic form of amisulpride which is under development for the treatment of bipolar depression. [ 1 ] [ 2 ] [ 3 ] It is taken by mouth . [ 1 ]
Low doses of amisulpride likewise showed anti-anhedonia-like effects. [5] ENX-104 is not expected to induce motor side effects like extrapyramidal symptoms (EPS) or catalepsy at the low doses employed, as these effects require higher occupancy of the D 2 receptor (e.g., ~80%). [5] ENX-104 is highly potent as a dopamine receptor antagonist. [5]
Lower doses, however, act upon dopamine autoreceptors, resulting in increased dopamine transmission, improving the negative symptoms of schizophrenia. Lower doses of amisulpride have also been shown to have antidepressant and anxiolytic effects in non-schizophrenic patients, leading to its use in dysthymia and social phobias.
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Neuroleptic-induced deficit syndrome is principally characterized by the same symptoms that constitute the negative symptoms of schizophrenia: emotional blunting, apathy, hypobulia, anhedonia, indifference, difficulty or total inability in thinking, difficulty or total inability in concentrating, lack of initiative, attention deficits, and desocialization. [2]