DT-Web

DB01425 - Alizapride


Identification
Name Alizapride
Accession Number DB01425
Type small molecule
Description Alizapride is a dopamine antagonist with prokinetic and antiemetic effects used in the treatment of nausea and vomiting, including postoperative nausea and vomiting.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 315.3702
Groups approved
Monoisotopic Weight 315.169524941
Pharmacology
Indication Alizapride is used in the treatment of nausea and vomiting, including postoperative nausea and vomiting.
Mechanism of action The anti-emetic action of Alizapride is due to its antagonist activity at D2 receptors in the chemoreceptor trigger zone (CTZ) in the central nervous system (CNS)--this action prevents nausea and vomiting triggered by most stimuli. Structurally similar to metoclopramide and, therefore, shares similar other atributres related to emesis and prokinetics.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination renal
Toxicity Not Available
Affected organisms Not Available
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
  • Szelenyi I, Herold H, Gothert M: Emesis induced in domestic pigs: a new experimental tool for detection of antiemetic drugs and for evaluation of emetogenic potential of new anticancer agents. J Pharmacol Toxicol Methods. 1994 Oct;32(2):109-16. - Pubmed
  • Gomez F, Ruiz P, Briceno F, Rivera C, Lopez R: Macrophage Fcgamma receptors expression is altered by treatment with dopaminergic drugs. Clin Immunol. 1999 Mar;90(3):375-87. - Pubmed
  • Dhasmana KM, Villalon CM, Zhu YN, Parmar SS: The role of dopamine (D2), alpha and beta-adrenoceptor receptors in the decrease in gastrointestinal transit induced by dopamine and dopamine-related drugs in the rat. Pharmacol Res. 1993 May-Jun;27(4):335-47. - Pubmed
  • Kilpatrick GJ, el Tayar N, Van de Waterbeemd H, Jenner P, Testa B, Marsden CD: The thermodynamics of agonist and antagonist binding to dopamine D-2 receptors. Mol Pharmacol. 1986 Sep;30(3):226-34. - Pubmed
DTHybrid score 0.2172

Predictions


Id Partner name Gene Name Score
23 D(1A) dopamine receptor DRD1 0.079
502 5-hydroxytryptamine 2A receptor HTR2A 0.0764
4119 Cytochrome P450 2D6 CYP2D6 0.0465
638 D(3) dopamine receptor DRD3 0.046
556 Alpha-1A adrenergic receptor ADRA1A 0.0384
320 5-hydroxytryptamine 1A receptor HTR1A 0.0363
432 D(4) dopamine receptor DRD4 0.0353
590 5-hydroxytryptamine 2C receptor HTR2C 0.0293
163 D(1B) dopamine receptor DRD5 0.0285
4512 Cytochrome P450 3A4 CYP3A4 0.0259
318 Alpha-2A adrenergic receptor ADRA2A 0.0233
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0224
632 Alpha-1B adrenergic receptor ADRA1B 0.0223
4200 Cytochrome P450 1A2 CYP1A2 0.0218
629 Alpha-2B adrenergic receptor ADRA2B 0.0217
378 Alpha-2C adrenergic receptor ADRA2C 0.0214
1588 Multidrug resistance protein 1 ABCB1 0.021
716 5-hydroxytryptamine 7 receptor HTR7 0.0175
436 5-hydroxytryptamine 2B receptor HTR2B 0.0174
725 5-hydroxytryptamine 1D receptor HTR1D 0.0171
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0155
885 5-hydroxytryptamine 1B receptor HTR1B 0.0154
492 Histamine H1 receptor HRH1 0.0148
6145 Solute carrier family 22 member 1 SLC22A1 0.0128
617 Muscarinic acetylcholine receptor M2 CHRM2 0.011
789 Alpha-1D adrenergic receptor ADRA1D 0.0105
465 Calmodulin CALM1 0.0102
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0101
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0098
6016 Cytochrome P450 2C19 CYP2C19 0.0093
4757 Cytochrome P450 2C9 CYP2C9 0.0092
1256 5-hydroxytryptamine 6 receptor HTR6 0.009
3876 Aromatic-L-amino-acid decarboxylase DDC 0.009
3923 Cholinesterase BCHE 0.009
4118 Cytochrome P450 3A5 CYP3A5 0.0089
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0088
750 Voltage-dependent calcium channel gamma-1 subunit CACNG1 0.0087
6107 Cytochrome P450 3A7 CYP3A7 0.0086
587 Serum albumin ALB 0.0084
5251 Carbonyl reductase [NADPH] 1 CBR1 0.0081
923 Glutamate receptor 3 GRIA3 0.0074
6013 Cytochrome P450 2E1 CYP2E1 0.0073
6030 Cytochrome P450 2B6 CYP2B6 0.0064
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0061
131 Synaptic vesicular amine transporter SLC18A2 0.006
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0055
4924 Cytochrome P450 2C8 CYP2C8 0.0055
824 Sodium-dependent serotonin transporter SLC6A4 0.0054
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0049
174 Sigma 1-type opioid receptor SIGMAR1 0.0048
921 Glutamate receptor 2 GRIA2 0.0045
528 5-hydroxytryptamine 1E receptor HTR1E 0.0042
6859 Protein S100-A4 S100A4 0.0041
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0041
94 5-hydroxytryptamine 4 receptor HTR4 0.004
6144 Solute carrier family 22 member 2 SLC22A2 0.004
694 Matrix protein 2 M 0.0039
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0036
380 Cytochrome P450 17A1 CYP17A1 0.0035
427 Substance-P receptor TACR1 0.0034
3939 Amine oxidase [flavin-containing] B MAOB 0.0034
341 5-hydroxytryptamine 3 receptor HTR3A 0.0033
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0031
1181 Alpha-1-acid glycoprotein 1 ORM1 0.003
3941 Amine oxidase [flavin-containing] A MAOA 0.0029
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0027
866 Large neutral amino acids transporter small subunit 2 SLC7A8 0.0024
6024 Cytochrome P450 1A1 CYP1A1 0.0024
245 Large neutral amino acids transporter small subunit 1 SLC7A5 0.0023
713 Sodium-dependent dopamine transporter SLC6A3 0.0022
3947 Xanthine dehydrogenase/oxidase XDH 0.002
124 Histamine H2 receptor HRH2 0.0018
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0018
6106 Cytochrome P450 2C18 CYP2C18 0.0018
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0018
474 Acetylcholinesterase ACHE 0.0018
15 Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I 0.0018
20 Prostaglandin G/H synthase 1 PTGS1 0.0017
535 Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G 0.0017
6151 Monocarboxylate transporter 10 SLC16A10 0.0016
464 Glutamate [NMDA] receptor subunit epsilon-2 GRIN2B 0.0016
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0016
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.0016
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0015
5718 Cytochrome P450 2A6 CYP2A6 0.0015
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
153 Dopamine beta-hydroxylase DBH 0.0014
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0013
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0012
3810 Catechol O-methyltransferase COMT 0.0012
776 Bile salt export pump ABCB11 0.0011
6147 Solute carrier family 22 member 3 SLC22A3 0.001
118 Organic cation/carnitine transporter 2 SLC22A5 0.0009
164 Histamine H4 receptor HRH4 0.0008
193 Beta-1 adrenergic receptor ADRB1 0.0008
766 Beta-2 adrenergic receptor ADRB2 0.0008
1898 Cytochrome P450 1B1 CYP1B1 0.0005
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