Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
369.172227057
InChI
InChI=1S/C17H27N3O4S/c1-4-20-8-6-7-12(20)11-19-17(21)13-9-16(25(22,23)5-2)14(18)10-15(13)24-3/h9-10,12H,4-8,11,18H2,1-3H3,(H,19,21)
InChI Key
InChIKey=NTJOBXMMWNYJFB-UHFFFAOYSA-N
IUPAC Name
4-amino-5-(ethanesulfonyl)-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxybenzamide
Traditional IUPAC Name
amisulpride
SMILES
CCN1CCCC1CNC(=O)C1=CC(=C(N)C=C1OC)S(=O)(=O)CC
pKa (strongest acidic)
14.03
pKa (Strongest Basic)
7.05
Refractivity
99.84 m3·mol-1
Cơ Chế Tác Dụng :
Amisulpride (trade name Solian) is an antipsychotic drug sold by Sanofi-Aventis. It is not approved for use in the United States, but is approved for use in Europe and Australia for the treatment of psychoses and schizophrenia. Additionally, it is approved in Italy for the treatment of dysthymia (under the brand name Deniban). Amisulpride is a selective dopamine antagonist.
Amisulpride binds selectively to dopamine D(2) and D(3) receptors in the limbic system. Low doses of amisulpride preferentially block presynaptic D(2)/D(3)-dopamine autoreceptors, thereby enhancing dopaminergic transmission, whereas higher doses block postsynaptic receptors, thus inhibiting dopaminergic hyperactivity. It may also have 5-ht7 antagonistic effect, useful in depression treatment.
Dược Động Học :
▧ Absorption :
Bioavailability is 48% following oral administration.
▧ Protein binding :
Low (17%)
▧ Half Life :
Approximately 12 hours
Độc Tính :
Overdoses of amisulpride have been linked with torsades de pointes.
Chỉ Định :
Investigated for use/treatment in schizophrenia and schizoaffective disorders, mania in bipolar disorder, and depression.