Carbamic acid,N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]-,methyl ester
- Product Name
- Carbamic acid,N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]-,methyl ester
- CAS No.
- 158364-59-1
- Chemical Name
- Carbamic acid,N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]-,methyl ester
- Synonyms
- PUMAPRAZOLE;Pumaprazole, 10 mM in DMSO;inhibit,Proton Pump,BY 841,Pumaprazole,BY841,Inhibitor;Methyl (2-(((2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino)methyl)-3-methylphenyl)carbamate;Carbamic acid,N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]-,methyl ester
- CBNumber
- CB33285508
- Molecular Formula
- C19H22N4O2
- Formula Weight
- 338.4
- MOL File
- 158364-59-1.mol
Carbamic acid,N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]-,methyl ester Property
- Density
- 1.21±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- pka
- 13.67±0.70(Predicted)
- color
- Light yellow to yellow
Carbamic acid,N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]-,methyl ester Chemical Properties,Usage,Production
Description
Pumaprazole has been abandoned in favor of a pharmacologically better follow up compound presently under development at Byk Gulden. The WHO decided to label the APAs by the stem syllable “-prazole” in order “to maintain the number of stems at a manageable level”, irrespective of the completely different (i.e., reversible vs. covalent) modes of drug – target interactions by APAs and PPIs (WHO decision communicated on Nov. 30, 1995). Unfortunately, this pharmacologically misleading but legally binding decision will confuse the rational use and differential perception of APAs vs. PPIs in the future and counteracts the effort for an unambiguous terminology in pharmacology. It should be noted that the terms APAs and PPIs have been coined specifically to make a clearly recognizable distinction between the two chemically and mechanistically different classes of drugs.
Uses
Pumaprazole is a reversible proton pump antagonist.
in vivo
Pumaprazole is a reversible proton pump antagonist. Basal acid secretion in the Ghosh-Schild rat is inhibited by Pumaprazole with a higher efficacy compare to ranitidine. Pumaprazole displays identical ID50 values on day 1 (11 μmol/kg, 95% confidence limits of 5 and 23) and on day 7 (10 μmol/kg, 95% confidence limits of 4 and 23) of a repeated dose study in this model. The lower dose of Pumaprazole (27 μmol/kg) rapidly elevates luminal pH up to almost neutrality, the higher dose (54 μmol/kg) further prolongs this pH-elevating effect[1].
References
[1] Kromer W, et al. Animal pharmacology of reversible antagonism of the gastric acid pump, compared to standard antisecretory principles. Pharmacology. 2000 May;60(4):179-87. DOI:10.1159/000028367
Carbamic acid,N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]-,methyl ester Preparation Products And Raw materials
Raw materials
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