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| Targets |
Cinitapride's mechanism of action involves the modulation of serotonin receptors. It is a 5-HT4 receptor agonist and a 5-HT2A receptor antagonist. By acting as a 5-HT4 agonist, it enhances the release of acetylcholine in the enteric nervous system, which increases gastrointestinal motility. Its 5-HT2A antagonistic activity may contribute to its effects by reducing inhibitory signals. This dual mechanism leads to improved gastric emptying and intestinal transit, making it effective for treating disorders like GERD and dyspepsia.
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| ln Vitro |
In vitro, Cinitapride has been shown to enhance gastrointestinal motility. Its activity is typically measured using isolated tissue preparations, such as the guinea pig ileum or rat stomach. In these assays, Cinitapride induces contractions or enhances the response to electrical stimulation, confirming its prokinetic activity. Its affinity for 5-HT4 and 5-HT2A receptors has been confirmed in receptor binding studies. However, specific IC50 or EC50 values are not detailed in standard product descriptions.
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| ln Vivo |
In a rat model of gastric ulcer, cipipride (ip; 0.25–1 mg/kg; once) exhibits gastroprotective benefits [2].
In vivo, Cinitapride has been shown to improve gastrointestinal motility and to be effective in treating GERD, non-ulcer dyspepsia, and delayed gastric emptying. It is marketed in several countries for these indications. Clinical studies have demonstrated its efficacy in reducing symptoms of these disorders. However, specific in vivo protocols and results are not detailed in standard product descriptions. Its use is established in clinical practice in some regions. |
| Enzyme Assay |
The in vitro assays for Cinitapride measure its binding to 5-HT4 and 5-HT2A receptors and its functional effects on gastrointestinal motility. Receptor binding assays are performed using membranes from cells expressing the receptors and radiolabeled ligands. Functional assays measure the compound's ability to stimulate contractions in isolated tissue preparations, such as the guinea pig ileum. The concentration-response curve is generated, and the EC50 is determined. These assays confirm Cinitapride's activity as a 5-HT4 agonist and 5-HT2A antagonist.
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| Cell Assay |
In vitro cell-based assays for Cinitapride are not typically performed, as its mechanism of action is primarily through receptor modulation in the enteric nervous system. However, its effects on receptor signaling can be studied using cells expressing 5-HT4 or 5-HT2A receptors. For example, the stimulation of cAMP production via 5-HT4 receptor activation can be measured. These cell-based assays confirm its activity at the receptor level.
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| Animal Protocol |
Animal/Disease Models: Male gastric ulcer Wistar rat [2]
Doses: 0.25-1 mg/kg Route of Administration: intraperitoneal (ip) injection; 0.25-1 mg/kg; Experimental Results: Compared with the ulcer control group, the bleeding lesions were diminished. At the highest dose (1 mg/kg), the ulcer percentage was diminished to 28.76%. Attenuated the increase in myeloperoxidase activity (p<0.05, p<0.01). GSH-px activity is increased in the gastric mucosa. In vivo animal experiments for Cinitapride are conducted in animal models of gastrointestinal motility disorders. In a typical study, rodents are treated with Cinitapride, and gastric emptying or intestinal transit is measured. The compound's ability to enhance motility is assessed. These studies confirm its prokinetic activity. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Oral administration of cilipride (12 mg) results in rapid absorption, reaching peak concentration 2 hours after administration; intramuscular administration (4 mg) results in even faster absorption, reaching peak concentration 1 hour after administration (50% higher than oral concentration). Biological Half-Life The half-life is 3-5 hours within the first 8 hours after administration, and thereafter the residual half-life is greater than 15 hours. Cinitapride has a molecular weight of 402.49 g/mol and a molecular formula of C21H30N4O4. It is a solid compound with a purity of typically NLT 98%. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been studied in the context of clinical use. However, specific values are not detailed in standard product descriptions. |
| Toxicity/Toxicokinetics |
Cinitapride is an approved drug in several countries and its safety profile has been established. Common side effects may include gastrointestinal disturbances, headache, and dizziness. As with all drugs, it should be used under medical supervision. It is contraindicated in patients with hypersensitivity to the drug. In research settings, standard laboratory safety precautions should be followed when handling Cinitapride.
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| References |
[1]. Du Y, et al. Efficacy and safety of cinitapride in the treatment of mild to moderate postprandial distress syndrome-predominant functional dyspepsia. J Clin Gastroenterol. 2014 Apr;48(4):328-35.
[2]. Alarcón de la Lastra C, et al. Effects of cinitapride on gastric ulceration and secretion in rats. Inflamm Res. 1998 Mar;47(3):131-6. [3]. Alarcón-de-la-Lastra Romero C, et al. 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. |
| Additional Infomation |
Cinitapride is an aromatic ether and C-nitro compound. It is a prokinetic and anti-ulcer benzamide drug with agonistic activity against 5-HT1 and 5-HT4 receptors and antagonistic activity against 5-HT2 receptors. It is marketed in Spain and Mexico. Indications: It is indicated for the treatment of gastrointestinal disorders associated with gastric motility disorders, such as gastroesophageal reflux disease (GERD), non-ulcer dyspepsia, and delayed gastric emptying. Mechanism of Action: Cinitapride is a substituted benzamide drug with both 5-HT receptor antagonistic and agonistic activity.
Cinitapride is a gastroprokinetic agent and antiulcer drug of the benzamide class. It is indicated for the treatment of gastrointestinal disorders associated with motility disturbances, such as GERD, non-ulcer dyspepsia, and delayed gastric emptying. It is marketed in several countries including India, Mexico, Pakistan, and Spain. Its mechanism of action involves 5-HT4 receptor agonism and 5-HT2A receptor antagonism. Cinitapride is an approved drug in some regions and is also used as a research compound. |
| Molecular Formula |
C21H30N4O4
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| Molecular Weight |
402.49
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| Exact Mass |
402.226
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| CAS # |
66564-14-5
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| Related CAS # |
66564-14-5;1207859-16-2 (tartrate);67135-13-1 (H tartrate);
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| PubChem CID |
68867
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
579.8±50.0 °C at 760 mmHg
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| Flash Point |
304.5±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.603
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| LogP |
3.87
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
586
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC1=CC(N)=C([N+]([O-])=O)C=C1C(NC1CCN(CC2CCC=CC2)CC1)=O
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| InChi Key |
ZDLBNXXKDMLZMF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H30N4O4/c1-2-29-20-13-18(22)19(25(27)28)12-17(20)21(26)23-16-8-10-24(11-9-16)14-15-6-4-3-5-7-15/h3-4,12-13,15-16H,2,5-11,14,22H2,1H3,(H,23,26)
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| Chemical Name |
4-amino-N-[1-(cyclohex-3-en-1-ylmethyl)piperidin-4-yl]-2-ethoxy-5-nitrobenzamide
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| Synonyms |
AS-17177Paxapride Cidine Blaston Cinmove Cintapro cinitapride tartrateAS 17177 AS17177Cinitapride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~20.83 mg/mL (~51.75 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4845 mL | 12.4227 mL | 24.8453 mL | |
| 5 mM | 0.4969 mL | 2.4845 mL | 4.9691 mL | |
| 10 mM | 0.2485 mL | 1.2423 mL | 2.4845 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT01355276
Conditions:DyspepsiaProducts are for research use only; We do not sell to patients
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