Chemistry:Cinitapride

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Cinitapride (trade names Cintapro, Pemix, Gapulsid) is a gastroprokinetic agent and antiemetic agent of the benzamide class which is marketed in India, Mexico, Pakistan, Spain,[1][2] Croatia and the Czech Republic. It acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors.[3][4]

Uses

It is indicated for the treatment of gastrointestinal disorders associated with motility disturbances such as gastroesophageal reflux disease, non-ulcer dyspepsia and delayed gastric emptying. It may be also used in the management of nausea and vomiting. Cinitapride works by increasing the movement of esophagus, stomach, and intestines during digestion. It also increases the strength of muscle between esophagus and stomach to prevent reflux conditions.

Synthesis

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Cinitapride is the amide formed by reacting methyl 4-amino-2-ethoxy-5-nitrobenzoate (1) with the 4-aminopiperidine derivative (2).[5][6]

References

  1. ↑ "The prokinetic cinitapride has no clinically relevant pharmacokinetic interaction and effect on QT during coadministration with ketoconazole". Drug Metabolism and Disposition 35 (7): 1149–56. July 2007. doi:10.1124/dmd.106.010835. PMID 17437965. http://dmd.aspetjournals.org/cgi/pmidlookup?view=long&pmid=17437965. 
  2. ↑ "Peripheral receptor populations involved in the regulation of gastrointestinal motility and the pharmacological actions of metoclopramide-like drugs". Life Sciences 36 (1): 1–14. January 1985. doi:10.1016/0024-3205(85)90280-2. PMID 2981378. 
  3. ↑ "Cinitapride protects against ethanol-induced gastric mucosal injury in rats: role of 5-hydroxytryptamine, prostaglandins and sulfhydryl compounds". Pharmacology 54 (4): 193–202. April 1997. doi:10.1159/000139487. PMID 9211565. 
  4. ↑ "Effects of cinitapride on gastric ulceration and secretion in rats". Inflammation Research 47 (3): 131–6. March 1998. doi:10.1007/s000110050301. PMID 9562338. http://link.springer-ny.com/link/service/journals/00011/bibs/8047003/80470131.htm. Retrieved 2010-02-27. 
  5. ↑ Inglesias, J.B; Soto, J.P; Noverola, A.V; Mauri, J.M, "Piperidine compounds", GB patent 1574419, issued 1980-09-03, assigned to Anphar SA
  6. ↑ "Cinitapride". Thieme. https://pharmaceutical-substances.thieme.com/ps/search-results?docUri=KD-03-0165. 



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