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Metabolism Studies of Ifenprodil, a Potent GluN2B Receptor Antagonist

Metabolism Studies of Ifenprodil, a Potent GluN2B Receptor Antagonist

Evamaria Falck, Frank Begrow, Eugen Verspohl, Bernhard Wünsch

J Pharm Biomed Anal. 2014 Jan;88:96-105.

PMID: 24042122

Abstract:

The NMDA receptor antagonist ifenprodil is an important lead structure for developing new GluN2B selective NMDA receptor antagonists. Ifenprodil itself has a high affinity to the GluN2B subunit but a poor selectivity for the NMDA receptor. This aspect and the fast biotransformation are the major drawbacks of ifenprodil. In order to optimize the development of new and more selective GluN2B (NMDA) receptor antagonists, the identification of the main metabolic pathways of ifenprodil is necessary. Herein the in vitro and in vivo phase I and phase II metabolites of ifenprodil were generated and analyzed via LC-MS(n) experiments. In vitro experiments were carried out with rat liver microsomes and various co-factors to generate phase I and phase II metabolites. The application of ifenprodil to a rat and the analysis of its urine led to the identification of diverse formed in vivo metabolites. The phenol represents the metabolically most labile structural element since glucuronide 7 and 8 appeared as main metabolites.

Chemicals Related in the Paper:

Catalog Number	Product Name	CAS Number	Price
AP109434211	Adenosine 3′-phosphate 5′-phosphosulfate lithium salt hydrate	109434-21-1	Price
AP23210584	Ifenprodil (+)-tartrate salt	23210-58-4	Price
AP63700196	Uridine 5′-diphosphoglucuronic acid trisodium salt	63700-19-6	Price

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