Wiki:
N-Methylamisulpride (developmental code name LB-102 ) is a dopamine D2 and D3 receptorantagonist and serotonin 5-HT2B and 5-HT7receptor antagonist which is under development for the treatment of schizophrenia.[1][2][3][4][5] It is a benzamide derivative and is the N -methylatedanalogue of amisulpride.[1][2] The drug is being developed for use both orally and parenterally.[1]
Amisulpride exhibits low passive diffusion through the blood–brain barrier and this requires higher doses for central nervous system activity.[2] N-Methylamisulpride has enhanced lipophilicity and hence improved passive diffusion through biological membranes like the blood–brain barrier compared to amisulpride.[2] This in turn is expected to provide a higher ratio of brain to peripheral concentrations.[2] The drug otherwise has similar pharmacodynamics and pharmacokinetics relative to amisulpride.[2][5]
N-Methylamisulpride appears to have considerably greater clinical potency compared to amisulpride owing to its improved lipophilicity and blood–brain barrier permeability.[2] A dosage of 50 mg/day N-methylamisulpride has been found to achieve 60 to 80% occupancy of the dopamine D2 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.[7][8][9] Due to its greater ratio of brain to peripheral concentrations and much lower doses, N-methylamisulpride is expected to have reduced risk of QT prolongation in comparison.[9][4]
As of December 2023, N-methylamisulpride is in phase 2 clinical trials for schizophrenia.[1] It is being developed by LB Pharmaceuticals.[1]
Amisulpride is such a good med. I was on it for couple of months and I felt great. Bad thing is that it incresed my prolactin levels. If LB-102 is as good as amisulpride but without the prolactin issue, it will be a big step forward.