Chemistry:Ifenprodil

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Ifenprodil, sold under the brand names Cerocral, Dilvax, and Vadilex, is a cerebral vasodilator that has been marketed in some countries, including in Japan, Hong Kong, and France.[1][2][3][4] It is currently under development for treatment of a variety of additional indications.[5]

Ifenprodil has multiple known pharmacological actions.[5] It is an inhibitor of the NMDA receptor,[6] specifically of NMDA receptors containing GluN1 and GluN2B subunits, the "ifenprodil binding site".[7] Additionally, ifenprodil inhibits GIRK channels[8] and interacts with α1-adrenergic,[5] serotonin,[9] and sigma receptors.[10][11][12][5]

Chemically, ifenprodil is a substituted phenethylamine and β-hydroxyamphetamine derivative.[2][3] It is used pharmaceutically as the tartrate salt.[1][2][3]

Research

Ifenprodil has been studied as a possible medication to prevent tinnitus after acoustic trauma.[13]

It is currently in phase II trials for cough and idiopathic pulmonary fibrosis, among other investigational uses.[5]

See also

  • Traxoprodil (another β-hydroxyamphetamine NMDA receptor antagonist)

References

  1. ↑ 1.0 1.1 The Merck Index (Thirteenth ed.). Whitehouse Station, NJ: Merck Research Laboratories Division of Merck & Co., Inc.. 2001. p. 878. 
  2. ↑ 2.0 2.1 2.2 The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer US. 2014. p. 676. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA676. Retrieved 2 September 2024. 
  3. ↑ 3.0 3.1 3.2 Schweizerischer Apotheker-Verein (2004). Index Nominum: International Drug Directory. Medpharm Scientific Publishers. p. 625. ISBN 978-3-88763-101-7. https://books.google.com/books?id=EgeuA47Ocm4C&pg=PA625. Retrieved 2 September 2024. 
  4. ↑ Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Netherlands. 2012. p. 150. ISBN 978-94-011-4439-1. https://books.google.com/books?id=tsjrCAAAQBAJ&pg=PA150. Retrieved 2 September 2024. 
  5. ↑ 5.0 5.1 5.2 5.3 5.4 "Ifenprodil - Algernon Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800055643. 
  6. ↑ "Ifenprodil is a novel type of N-methyl-D-aspartate receptor antagonist: interaction with polyamines". Molecular Pharmacology 36 (5): 758–765. November 1989. doi:10.1016/S0026-895X(25)09662-2. PMID 2555674. 
  7. ↑ "Neurosteroid modulation of N-methyl-D-aspartate receptors: molecular mechanism and behavioral effects". Steroids 76 (13): 1409–1418. December 2011. doi:10.1016/j.steroids.2011.09.002. PMID 21925193. 
  8. ↑ "Inhibition of G protein-activated inwardly rectifying K+ channels by ifenprodil". Neuropsychopharmacology 31 (3): 516–524. March 2006. doi:10.1038/sj.npp.1300844. PMID 16123769. 
  9. ↑ "Ifenprodil inhibition of the 5-hydroxytryptamine3 receptor". Neuropharmacology 34 (6): 621–629. June 1995. doi:10.1016/0028-3908(95)00030-a. PMID 7566498. 
  10. ↑ "Further characterization of [3H]ifenprodil binding to sigma receptors in rat brain". European Journal of Pharmacology 236 (1): 159–163. May 1993. doi:10.1016/0014-2999(93)90241-9. PMID 8319742. 
  11. ↑ "Further characterization of [3H]ifenprodil binding in rat brain". European Journal of Pharmacology 266 (1): 67–77. January 1994. doi:10.1016/0922-4106(94)90211-9. PMID 7907988. 
  12. ↑ "Interactions of erythro-ifenprodil, threo-ifenprodil, erythro-iodoifenprodil, and eliprodil with subtypes of sigma receptors". European Journal of Pharmacology 273 (3): 307–310. February 1995. doi:10.1016/0014-2999(94)00763-w. PMID 7737340. 
  13. ↑ "Blockade of cochlear NMDA receptors prevents long-term tinnitus during a brief consolidation window after acoustic trauma". Neural Plasticity (Hindawi Limited) 2007. 2007. doi:10.1155/2007/80904. PMID 18301716. 



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