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Pharmacological and metabolic characterisation of the potent sigma 1 receptor ligand 1'-benzyl-3-methoxy-3H-spiro[[2]benzofuran-1,4'-piperidine]
Journal of Pharmacy and Pharmacology, 05/05/09

Wiese C et al. - Studies with seven recombinant cytochrome P450 isoenzymes revealed that CYP3A4 produced all the metabolites identified. The isoenzyme CYP2D6 was inhibited by 1 but did not produce any metabolites. 1'-Benzyl-3-methoxy-3H-spiro[[2]benzofuran-1,4'-piperidine] is a potent and selective sigma 1 receptor antagonist, which is rapidly metabolised. Metabolically more stable sigma 1 ligands could be achieved by stabilising the N-benzyl substructure.

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UGT1A10: Activity against the tobacco-specific nitrosamine, NNAL, and a potential role for a novel UGT1A10 promoter deletion polymorphism in cancer susceptibility
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Glucuronidation of Psilocin and 4-Hydroxyindole by the Human UDP-glucuronosyltransferases
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Evaluation of Treatment Satisfaction in Children with Allergic Disease Treated with an Antihistamine: An International, Non-Interventional, Retrospective Study
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Sanofi Pasteur Global Dengue Vaccine Clinical Program Expanded in Latin America
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