Clebopride Malate - CAS 57645-91-7
Catalog number: 57645-91-7
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C23H28ClN3O6
Molecular Weight:
477.94
COA:
Inquire
Targets:
Dopamine Receptor
Description:
Clebopride is a substituted benzamide as a dopamine antagonist used to treat functional gastrointestinal disorders.
Purity:
≥95%
Appearance:
White to off-white solid
Synonyms:
4-Amino-5-chloro-2-methoxy-N-(1-benzyl-4-piperidyl)benzamide malate; 4-amino-N-(1-benzylpiperidin-1-ium-4-yl)-5-chloro-2-methoxybenzamide;2,4-dihydroxy-4-oxobutanoate;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
Dopamine antagonist
Quality Standard:
Enterprise Standard/EP/BP/GP
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Grams-Kilos
InChIKey:
NYNKCGWJPNZJMI-UHFFFAOYSA-N
InChI:
1S/C20H24ClN3O2.C4H6O5/c1-26-19-12-18(22)17(21)11-16(19)20(25)23-15-7-9-24(10-8-15)13-14-5-3-2-4-6-14;5-2(4(8)9)1-3(6)7/h2-6,11-12,15H,7-10,13,22H2,1H3,(H,23,25);2,5H,1H2,(H,6,7)(H,8,9)
Canonical SMILES:
COC1=CC(=C(C=C1C(=O)NC2CC[NH+](CC2)CC3=CC=CC=C3)Cl)N.C(C(C(=O)[O-])O)C(=O)O
1.A phase I trial of a new antiemetic drug--clebopride malate--in cisplatin-treated patients.
Bleiberg H1, Piccart M, Lips S, Panzer JM, N'Koua Mbon JB. Ann Oncol. 1992 Feb;3(2):141-3.
Clebopride, a new benzamide derivative, has, in common with the other members of this group, antidopaminergic activity. In animals, its therapeutic ratio is superior to that of metoclopramide at doses free of side effects associated with hyperprolactinemia and extrapyramidal symptoms. The present study was designed to define the maximum tolerated dose (MTD) in patients with advanced histologically-proven cancer, treated with cisplatin at a dose of greater than 50 mg/m2. Most of them were pretreated and refractory to standard antiemetics. Clebopride was started at a dosage of 0.10 mg/kg in a group of 6 patients and escalated by 0.2 mg at each dose level. A total of 30 patients were included. Side effects include somnolence, diarrhea and extrapyramidal-like symptoms. The latter occurred at almost all dose levels in 14% of the cycles and limited continuation of the study. Activity in this group of patients was encouraging but, considering the rate of extrapyramidal symptoms, further dose escalation is not indicated and activity at lower, nontoxic levels should be investigated.
2.Determination of clebopride in plasma by capillary gas chromatography-negative-ion chemical ionization mass spectrometry.
Robinson PR1, Jones MD, Maddock J. J Chromatogr. 1988 Nov 18;432:153-63.
A procedure for the analysis of clebopride in plasma using capillary gas chromatography-negative-ion chemical ionization mass spectrometry has been developed. Employing an ethoxy analogue as internal standard, the two compounds were extracted from basified plasma using dichloromethane. Subsequent reaction with heptafluorobutyryl imidazole produced volatile monoheptafluorobutyryl derivatives whose ammonia negative-ion mass spectra proved ideal for selected-ion monitoring. The recovery of clebopride from plasma at 0.536 nmol/l was found to be 85.5 +/- 0.9% (n = 3) whilst measurement down to 0.268 nmol/l was possible with a coefficient of variation of 7.9%. Plasma levels of the compound are reported in two volunteers following ingestion of 1 mg of clebopride as the malate salt.
3.Partial least-squares regression for the quantitation of pharmaceutical dosages in control analyses.
Blanco M1, Coello J, Elaamrani M, Iturriaga H, Maspoch S. J Pharm Biomed Anal. 1996 Dec;15(3):329-38.
A spectrophotometric method for the simultaneous determination of the active principle and a flavouring agent in syrups containing additional excipients is proposed. The calibration matrix must include all the variability expected in the samples and this is achieved using laboratory-made mixtures and production samples in order to ensure correct results. The optimum number of principal components for the regression model was selected by using various procedures. The proposed method was used to quantify samples from different production batches. The results are compared with those provided by HPLC.
4.Simultaneous determination of clebopride and a major metabolite N-desbenzylclebopride in plasma by capillary gas chromatography-negative-ion chemical ionization mass spectrometry.
Robinson PR1, Jones MD, Maddock J, Rees LW. J Chromatogr. 1991 Mar 8;564(1):147-61.
A procedure for the simultaneous assay of clebopride and its major metabolite N-desbenzylclebopride in plasma has been developed. The method utilizes capillary gas chromatography-negative-ion chemical ionization mass spectrometry with selected-ion monitoring of characteristic ions. Employing 2-ethoxy analogues as internal standards, the benzamides were extracted from basified plasma using dichloromethane. Subsequent reaction with heptafluorobutyric anhydride produced volatile mono- and diheptafluorobutyryl derivatives of clebopride and N-desbenzylclebopride, respectively. The methane negative-ion mass spectra of these derivatives exhibited intense high-mass ions ideal for specific quantitation of low levels in biological fluids. Using this procedure the recovery of the drug and metabolite from human plasma was found to be 84.4 +/- 1.5% (n = 3) and 77.4 +/- 4.7% (n = 3), respectively, at 0.5 ng/ml. Measurement of both compounds down to 0.
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Chemical Structure

CAS 57645-91-7 Clebopride Malate

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