Can silicon make an excellent drug even better? An in vitro and in vivo head-to-head comparison between loperamide and its silicon analogue sila-loperamide.

Geyer, Marcel; Wellner, Eric; Jurva, Ulrik; Saloman, Sebastian; Armstrong, Duncan; Tacke, Reinhold

Geyer, Marcel; Wellner, Eric; Jurva, Ulrik; Saloman, Sebastian; Armstrong, Duncan; Tacke, Reinhold.

Affiliation

Geyer M; Universität Würzburg, Institut für Anorganische Chemie, Am Hubland, 97074 Würzburg (Germany).

ChemMedChem ; 10(5): 911-24, 2015 May.

Article in En | MEDLINE | ID: mdl-25801200

Subject(s)

Cytochrome P-450 Enzyme System/metabolism; Enzyme Inhibitors/chemistry; Enzyme Inhibitors/pharmacology; Loperamide/analogs & derivatives; Loperamide/pharmacology; Organosilicon Compounds/chemical synthesis; Organosilicon Compounds/pharmacology; Animals; Cell Line; Cricetulus; Dose-Response Relationship, Drug; Enzyme Inhibitors/chemical synthesis; Hepatocytes/chemistry; Hepatocytes/metabolism; Humans; Loperamide/chemistry; Male; Microsomes, Liver/chemistry; Microsomes, Liver/metabolism; Molecular Structure; Organosilicon Compounds/chemistry; Rats; Rats, Wistar; Structure-Activity Relationship

Key words

C/Si exchange; metabolic fate; opioid receptors; sila-drugs; silicon

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Full text: 1 Database: MEDLINE Main subject: Organosilicon Compounds / Cytochrome P-450 Enzyme System / Enzyme Inhibitors / Loperamide Type of study: Prognostic_studies Limits: Animals / Humans / Male Language: En Journal: ChemMedChem Journal subject: FARMACOLOGIA / QUIMICA Year: 2015 Type: Article

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