Veralipride - CAS 66644-81-3
Category: Inhibitor
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Molecular Formula:
C17H25N3O5S
Molecular Weight:
383.46
COA:
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Targets:
Dopamine Receptor
Description:
Veralipride is a D2 receptor antagonist in the hypothalamic system and has a half-life of approximately 12 hours. Veralipride is highly active on the neurotransmitters, producing both a weak blockade of the central postsynaptic dopaminergic receptors and particularly a strong blockade of the dopamine receptors in the hypothalamic nuclei.
Brife Description:
A D2 receptor antagonist
Synonyms:
LIR 1660, LIR-1660, LIR1660, Veralipride, Agreal, Agradil; 2,3-dimethoxy-N-[(1-prop-2-enylpyrrolidin-2-yl)methyl]-5-sulfamoylbenzamide; Agréal; Agreal; Menofel; N-(1-allyl-2-pyrrolidinyl)methyl-2,3-dimethoxy-5-sulfamoylbenzamide; Veraligral; veralipride; veralipride monohydrochloride
Solubility:
DMSO: ≥ 100 mg/mL
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
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Density:
1.230±0.06 g/cm3
InChIKey:
RYJXBGGBZJGVQF-UHFFFAOYSA-N
InChI:
1S/C17H25N3O5S/c1-4-7-20-8-5-6-12(20)11-19-17(21)14-9-13(26(18,22)23)10-15(24-2)16(14)25-3/h4,9-10,12H,1,5-8,11H2,2-3H3,(H,19,21)(H2,18,22,23)
Canonical SMILES:
COC1=C(C(=CC(=C1)S(=O)(=O)N)C(=O)NCC2CCCN2CC=C)OC
1.Improved determination of sulpiride in plasma by ion-pair liquid chromatography with fluorescence detection.
Nicolas P;Fauvelle F;Ennachachibi A;Merdjan H;Petitjean O J Chromatogr. 1986 Sep 5;381(2):393-400.
A specific and sensitive high-performance liquid chromatographic method for the measurement of sulpiride in plasma is described. The internal standard used was veralipride, a structurally related substituted benzamide. A fluorescence detector with maximum excitation at 300 nm and maximum emission at 365 nm was used for quantitation. After an alkaline extraction procedure, the benzamides were separated on a 5-micron ODS column using a large organic counter ion in the mobile phase. The detector response was linear from 10 to 1000 ng/ml and the detection limit was 10 ng/ml, which is sensitive enough for pharmacokinetic studies. The suitability of the method for the analysis of biological samples was tested by studying the variation with time of plasma concentrations of sulpiride in normal human volunteers after a single therapeutic 200-mg oral dose of three different formulations of sulpiride.
2.[The alternative to hormonal treatment of menopausal vasomotor flushes: veralipride].
Wesel S;Bosuma WB Sem Hop. 1983 Mar 3;59(9):596-9.
The effectiveness on hot flushes and clinical tolerance of veralipride were compared to those of natural estrogens in a randomized double blind trial. Forty-three patients who had undergone spontaneous menopause at least 6 months earlier were included in the study. For 20 days, twenty-one women were given 100 mg per day veralipride and twenty-two were given 1.25 mg of the reference estrogen. Three women in the estrogen group discontinued the trial without sound reasons. The number, duration and severity of hot flushes were assessed and scored at the onset of the trial and after 7 and 20 days of treatment. Statistical analysis showed no significant difference concerning effectiveness or tolerance. However, veralipride seemed to provide better control of severe hot flushes.
3.Adverse drug reactions in patients with phaeochromocytoma: incidence, prevention and management.
Eisenhofer G;Rivers G;Rosas AL;Quezado Z;Manger WM;Pacak K Drug Saf. 2007;30(11):1031-62.
The dangers of phaeochromocytomas are mainly due to the capability of these neuroendocrine tumours to secrete large quantities of vasoactive catecholamines, thereby increasing blood pressure and causing other related adverse events or complications. Phaeochromocytomas are often missed, sometimes only becoming apparent during therapeutic interventions that provoke release or interfere with the disposition of catecholamines produced by the tumours. Because phaeochromocytomas are rare, evidence contraindicating use of specific drugs is largely anecdotal or based on case reports. The heterogeneous nature of the tumours also makes adverse reactions highly variable among patients. Some drugs, such as dopamine D(2) receptor antagonists (e.g. metoclopramide, veralipride) and beta-adrenergic receptor antagonists (beta-blockers) clearly carry high potential for adverse reactions, while others such as tricyclic antidepressants seem more inconsistent in producing complications. Other drugs capable of causing adverse reactions include monoamine oxidase inhibitors, sympathomimetics (e.g. ephedrine) and certain peptide and corticosteroid hormones (e.g. corticotropin, glucagon and glucocorticoids).
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CAS 66644-81-3 Veralipride

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