DT-Web

DB06288 - Amisulpride


Identification
Name Amisulpride
Accession Number DB06288
Type small molecule
Description 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.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 369.479
Groups approved
Monoisotopic Weight 369.172227057
Pharmacology
Indication Investigated for use/treatment in schizophrenia and schizoaffective disorders, mania in bipolar disorder, and depression.
Mechanism of action 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.
Absorption Bioavailability is 48% following oral administration.
Protein binding Low (17%)
Biotransformation Not Available
Route of elimination Not Available
Toxicity Overdoses of amisulpride have been linked with torsades de pointes.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


D(2) dopamine receptor
Name D(2) dopamine receptor
Gene Name DRD2
Pharmacological action yes
Actions antagonist
References
  • Rosenzweig P, Canal M, Patat A, Bergougnan L, Zieleniuk I, Bianchetti G: A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers. Hum Psychopharmacol. 2002 Jan;17(1):1-13. - Pubmed
  • Horacek J, Bubenikova-Valesova V, Kopecek M, Palenicek T, Dockery C, Mohr P, Hoschl C: Mechanism of action of atypical antipsychotic drugs and the neurobiology of schizophrenia. CNS Drugs. 2006;20(5):389-409. - Pubmed
  • Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. - Pubmed
DTHybrid score 0.4184
D(3) dopamine receptor
Name D(3) dopamine receptor
Gene Name DRD3
Pharmacological action unknown
Actions antagonist
References
  • Rosenzweig P, Canal M, Patat A, Bergougnan L, Zieleniuk I, Bianchetti G: A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers. Hum Psychopharmacol. 2002 Jan;17(1):1-13. - Pubmed
  • Horacek J, Bubenikova-Valesova V, Kopecek M, Palenicek T, Dockery C, Mohr P, Hoschl C: Mechanism of action of atypical antipsychotic drugs and the neurobiology of schizophrenia. CNS Drugs. 2006;20(5):389-409. - Pubmed
  • Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. - Pubmed
DTHybrid score 0.2353
5-hydroxytryptamine 7 receptor
Name 5-hydroxytryptamine 7 receptor
Gene Name HTR7
Pharmacological action yes
Actions antagonist
References
  • Abbas AI, Hedlund PB, Huang XP, Tran TB, Meltzer HY, Roth BL: Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo. Psychopharmacology (Berl). 2009 Jul;205(1):119-28. Epub 2009 Apr 1. - Pubmed
DTHybrid score 0.1918
5-hydroxytryptamine 2A receptor
Name 5-hydroxytryptamine 2A receptor
Gene Name HTR2A
Pharmacological action unknown
Actions antagonist
References
  • Tyson PJ, Roberts KH, Mortimer AM: Are the cognitive effects of atypical antipsychotics influenced by their affinity to 5HT-2A receptors? Int J Neurosci. 2004 Jun;114(6):593-611. - Pubmed
DTHybrid score 0.3503

Predictions


Id Partner name Gene Name Score
23 D(1A) dopamine receptor DRD1 0.1949
320 5-hydroxytryptamine 1A receptor HTR1A 0.1694
590 5-hydroxytryptamine 2C receptor HTR2C 0.1514
4119 Cytochrome P450 2D6 CYP2D6 0.1412
432 D(4) dopamine receptor DRD4 0.139
318 Alpha-2A adrenergic receptor ADRA2A 0.1207
378 Alpha-2C adrenergic receptor ADRA2C 0.1161
556 Alpha-1A adrenergic receptor ADRA1A 0.1157
4512 Cytochrome P450 3A4 CYP3A4 0.1049
629 Alpha-2B adrenergic receptor ADRA2B 0.1012
163 D(1B) dopamine receptor DRD5 0.1004
436 5-hydroxytryptamine 2B receptor HTR2B 0.0998
725 5-hydroxytryptamine 1D receptor HTR1D 0.0912
885 5-hydroxytryptamine 1B receptor HTR1B 0.087
492 Histamine H1 receptor HRH1 0.0763
4200 Cytochrome P450 1A2 CYP1A2 0.0756
632 Alpha-1B adrenergic receptor ADRA1B 0.0748
1256 5-hydroxytryptamine 6 receptor HTR6 0.0643
1588 Multidrug resistance protein 1 ABCB1 0.063
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0629
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0468
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0454
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0446
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0431
4118 Cytochrome P450 3A5 CYP3A5 0.0395
528 5-hydroxytryptamine 1E receptor HTR1E 0.0391
6107 Cytochrome P450 3A7 CYP3A7 0.0377
789 Alpha-1D adrenergic receptor ADRA1D 0.0366
6016 Cytochrome P450 2C19 CYP2C19 0.0346
4757 Cytochrome P450 2C9 CYP2C9 0.0323
174 Sigma 1-type opioid receptor SIGMAR1 0.0292
341 5-hydroxytryptamine 3 receptor HTR3A 0.0286
6145 Solute carrier family 22 member 1 SLC22A1 0.0279
824 Sodium-dependent serotonin transporter SLC6A4 0.0264
6013 Cytochrome P450 2E1 CYP2E1 0.0256
6030 Cytochrome P450 2B6 CYP2B6 0.0222
540 Sodium-dependent noradrenaline transporter SLC6A2 0.022
587 Serum albumin ALB 0.0216
3923 Cholinesterase BCHE 0.0213
124 Histamine H2 receptor HRH2 0.0199
94 5-hydroxytryptamine 4 receptor HTR4 0.0185
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0178
750 Voltage-dependent calcium channel gamma-1 subunit CACNG1 0.0175
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0173
4924 Cytochrome P450 2C8 CYP2C8 0.0167
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0155
465 Calmodulin CALM1 0.0153
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0151
923 Glutamate receptor 3 GRIA3 0.0149
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0144
131 Synaptic vesicular amine transporter SLC18A2 0.0131
5251 Carbonyl reductase [NADPH] 1 CBR1 0.0131
713 Sodium-dependent dopamine transporter SLC6A3 0.0124
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0114
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0103
6144 Solute carrier family 22 member 2 SLC22A2 0.0102
5718 Cytochrome P450 2A6 CYP2A6 0.01
3941 Amine oxidase [flavin-containing] A MAOA 0.0097
921 Glutamate receptor 2 GRIA2 0.0092
3939 Amine oxidase [flavin-containing] B MAOB 0.0082
6024 Cytochrome P450 1A1 CYP1A1 0.0079
866 Large neutral amino acids transporter small subunit 2 SLC7A8 0.0075
474 Acetylcholinesterase ACHE 0.0072
511 5-hydroxytryptamine 1F receptor HTR1F 0.0072
245 Large neutral amino acids transporter small subunit 1 SLC7A5 0.007
193 Beta-1 adrenergic receptor ADRB1 0.0067
464 Glutamate [NMDA] receptor subunit epsilon-2 GRIN2B 0.0066
766 Beta-2 adrenergic receptor ADRB2 0.0066
20 Prostaglandin G/H synthase 1 PTGS1 0.0064
164 Histamine H4 receptor HRH4 0.0064
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0055
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.005
6151 Monocarboxylate transporter 10 SLC16A10 0.005
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0047
6147 Solute carrier family 22 member 3 SLC22A3 0.0044
153 Dopamine beta-hydroxylase DBH 0.0044
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0044
3426 Glutamine synthetase glnA 0.0043
3987 Glutamine synthetase GLUL 0.0043
6432 Transporter snf 0.0042
6859 Protein S100-A4 S100A4 0.0041
694 Matrix protein 2 M 0.0039
1898 Cytochrome P450 1B1 CYP1B1 0.0037
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0036
3810 Catechol O-methyltransferase COMT 0.0035
380 Cytochrome P450 17A1 CYP17A1 0.0035
427 Substance-P receptor TACR1 0.0034
118 Organic cation/carnitine transporter 2 SLC22A5 0.0033
6106 Cytochrome P450 2C18 CYP2C18 0.0032
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0031
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.003
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0027
696 Kappa-type opioid receptor OPRK1 0.0024
776 Bile salt export pump ABCB11 0.0023
3947 Xanthine dehydrogenase/oxidase XDH 0.002
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.002
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.002
1656 CYP2B protein CYP2B 0.0019
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0018
15 Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I 0.0018
535 Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G 0.0017
904 Glutathione S-transferase P GSTP1 0.0016
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.0016
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0015
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0015
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0014
1360 Sphingomyelin phosphodiesterase SMPD1 0.0014
833 Organic cation/carnitine transporter 1 SLC22A4 0.0014
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0012
1618 High affinity nerve growth factor receptor NTRK1 0.001
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0009
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0007
467 Delta-type opioid receptor OPRD1 0.0006
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