DT-Web

DB08810 - Cinitapride


Identification
Name Cinitapride
Accession Number DB08810
Type small molecule
Description Cinitapride is a gastroprokinetic agent and antiulcer agent of the benzamide class which is marketed in Spain and Mexico. It acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 402.4873
Groups approved
Monoisotopic Weight 402.226705468
Pharmacology
Indication For the treatment of gastrointestinal disorders associated with motility disturbances such as gastroesophageal reflux disease, non-ulcer dyspepsia and delayed gastric emptying.
Mechanism of action Cinitapride is a substituted benzamide with 5-HT receptor antagonist and agonist activity.
Absorption The absorption of cinitapride (12mg) following oral administration was rapid, with peak levels being achieved 2 h after dosing; absorption following intramuscular administration (4mg) was even more rapid, with peak levels (50% more that oral levels) being achieved 1 h after dosing.
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity The symptoms of overdose include drowsiness, confusion and extrapyramidal effects.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Atropine Anticholinergic agents like atropine may reduce the action of cinitapride.
Digoxin Cinitapride can alter the absorption of digoxin as it simulates gastric emptying.
Digoxin Immune Fab Cinitapride can alter the absorption of digoxin as it simulates gastric emptying.
Methylscopolamine Anticholinergic agents like methylscopolamine may reduce the action of cinitapride.
Scopolamine Anticholinergic agents like scopolamine may reduce the action of cinitapride.
Food Interactions Not Available

Targets


5-hydroxytryptamine 1A receptor
Name 5-hydroxytryptamine 1A receptor
Gene Name HTR1A
Pharmacological action yes
Actions agonist
References
  • Alarcon-de-la-Lastra Romero C, Lopez A, Martin MJ, la Casa C, Motilva V: Cinitapride protects against ethanol-induced gastric mucosal injury in rats: role of 5-hydroxytryptamine, prostaglandins and sulfhydryl compounds. Pharmacology. 1997 Apr;54(4):193-202. - Pubmed
  • Alarcon de la Lastra C, La Casa C, Martin MJ, Motilva V: Effects of cinitapride on gastric ulceration and secretion in rats. Inflamm Res. 1998 Mar;47(3):131-6. - Pubmed
DTHybrid score 0.2881
5-hydroxytryptamine 2A receptor
Name 5-hydroxytryptamine 2A receptor
Gene Name HTR2A
Pharmacological action yes
Actions antagonist
References
  • Alarcon-de-la-Lastra Romero C, Lopez A, Martin MJ, la Casa C, Motilva V: Cinitapride protects against ethanol-induced gastric mucosal injury in rats: role of 5-hydroxytryptamine, prostaglandins and sulfhydryl compounds. Pharmacology. 1997 Apr;54(4):193-202. - Pubmed
  • Alarcon de la Lastra C, La Casa C, Martin MJ, Motilva V: Effects of cinitapride on gastric ulceration and secretion in rats. Inflamm Res. 1998 Mar;47(3):131-6. - Pubmed
DTHybrid score 0.2866
5-hydroxytryptamine 4 receptor
Name 5-hydroxytryptamine 4 receptor
Gene Name HTR4
Pharmacological action unknown
Actions agonist
References
  • Alarcon-de-la-Lastra Romero C, Lopez A, Martin MJ, la Casa C, Motilva V: Cinitapride protects against ethanol-induced gastric mucosal injury in rats: role of 5-hydroxytryptamine, prostaglandins and sulfhydryl compounds. Pharmacology. 1997 Apr;54(4):193-202. - Pubmed
  • Alarcon de la Lastra C, La Casa C, Martin MJ, Motilva V: Effects of cinitapride on gastric ulceration and secretion in rats. Inflamm Res. 1998 Mar;47(3):131-6. - Pubmed
DTHybrid score 0.2582

Predictions


Id Partner name Gene Name Score
831 D(2) dopamine receptor DRD2 0.1429
4119 Cytochrome P450 2D6 CYP2D6 0.1194
590 5-hydroxytryptamine 2C receptor HTR2C 0.0978
23 D(1A) dopamine receptor DRD1 0.0815
885 5-hydroxytryptamine 1B receptor HTR1B 0.0792
4512 Cytochrome P450 3A4 CYP3A4 0.0754
4200 Cytochrome P450 1A2 CYP1A2 0.0675
436 5-hydroxytryptamine 2B receptor HTR2B 0.0663
556 Alpha-1A adrenergic receptor ADRA1A 0.0658
318 Alpha-2A adrenergic receptor ADRA2A 0.0658
638 D(3) dopamine receptor DRD3 0.0564
725 5-hydroxytryptamine 1D receptor HTR1D 0.0548
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0525
378 Alpha-2C adrenergic receptor ADRA2C 0.0503
716 5-hydroxytryptamine 7 receptor HTR7 0.0499
432 D(4) dopamine receptor DRD4 0.0487
824 Sodium-dependent serotonin transporter SLC6A4 0.0484
629 Alpha-2B adrenergic receptor ADRA2B 0.0473
4757 Cytochrome P450 2C9 CYP2C9 0.0452
632 Alpha-1B adrenergic receptor ADRA1B 0.0452
341 5-hydroxytryptamine 3 receptor HTR3A 0.0408
4118 Cytochrome P450 3A5 CYP3A5 0.0402
492 Histamine H1 receptor HRH1 0.04
6107 Cytochrome P450 3A7 CYP3A7 0.0384
163 D(1B) dopamine receptor DRD5 0.0354
6013 Cytochrome P450 2E1 CYP2E1 0.0353
1588 Multidrug resistance protein 1 ABCB1 0.0312
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0298
380 Cytochrome P450 17A1 CYP17A1 0.0294
193 Beta-1 adrenergic receptor ADRB1 0.0271
1256 5-hydroxytryptamine 6 receptor HTR6 0.0269
6016 Cytochrome P450 2C19 CYP2C19 0.0268
766 Beta-2 adrenergic receptor ADRB2 0.0266
4924 Cytochrome P450 2C8 CYP2C8 0.0262
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0257
540 Sodium-dependent noradrenaline transporter SLC6A2 0.023
274 Muscarinic acetylcholine receptor M5 CHRM5 0.022
6145 Solute carrier family 22 member 1 SLC22A1 0.0217
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0216
511 5-hydroxytryptamine 1F receptor HTR1F 0.0216
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0214
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0212
587 Serum albumin ALB 0.021
789 Alpha-1D adrenergic receptor ADRA1D 0.0199
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0188
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0175
3941 Amine oxidase [flavin-containing] A MAOA 0.0173
6030 Cytochrome P450 2B6 CYP2B6 0.0167
174 Sigma 1-type opioid receptor SIGMAR1 0.0146
847 Mu-type opioid receptor OPRM1 0.0144
5718 Cytochrome P450 2A6 CYP2A6 0.0136
528 5-hydroxytryptamine 1E receptor HTR1E 0.0126
713 Sodium-dependent dopamine transporter SLC6A3 0.0115
1517 Beta-3 adrenergic receptor ADRB3 0.0094
750 Voltage-dependent calcium channel gamma-1 subunit CACNG1 0.0089
923 Glutamate receptor 3 GRIA3 0.0075
131 Synaptic vesicular amine transporter SLC18A2 0.0071
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0069
6106 Cytochrome P450 2C18 CYP2C18 0.0068
124 Histamine H2 receptor HRH2 0.0067
474 Acetylcholinesterase ACHE 0.0055
6144 Solute carrier family 22 member 2 SLC22A2 0.0052
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0052
921 Glutamate receptor 2 GRIA2 0.0047
1656 CYP2B protein CYP2B 0.0044
3426 Glutamine synthetase glnA 0.0043
3987 Glutamine synthetase GLUL 0.0043
6432 Transporter snf 0.0042
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.004
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0037
6024 Cytochrome P450 1A1 CYP1A1 0.0033
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0032
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0032
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0032
20 Prostaglandin G/H synthase 1 PTGS1 0.0032
696 Kappa-type opioid receptor OPRK1 0.0032
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.003
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0029
3939 Amine oxidase [flavin-containing] B MAOB 0.0028
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0027
776 Bile salt export pump ABCB11 0.0027
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0025
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0025
3923 Cholinesterase BCHE 0.0025
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0024
1618 High affinity nerve growth factor receptor NTRK1 0.0023
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0021
164 Histamine H4 receptor HRH4 0.002
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0017
464 Glutamate [NMDA] receptor subunit epsilon-2 GRIN2B 0.0017
5251 Carbonyl reductase [NADPH] 1 CBR1 0.0017
904 Glutathione S-transferase P GSTP1 0.0016
465 Calmodulin CALM1 0.0015
467 Delta-type opioid receptor OPRD1 0.0014
1360 Sphingomyelin phosphodiesterase SMPD1 0.0014
833 Organic cation/carnitine transporter 1 SLC22A4 0.0014
6147 Solute carrier family 22 member 3 SLC22A3 0.0014
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0013
1898 Cytochrome P450 1B1 CYP1B1 0.0012
118 Organic cation/carnitine transporter 2 SLC22A5 0.0006
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