The Anxiolytic Etifoxine Binds to TSPO Ro5-4864 Binding Site with Long Residence Time Showing a High Neurosteroidogenic Activity

The low binding affinity of the approved anxiolytic drug etifoxine (Stresam) at the steroidogenic 18 kDa translocator protein (TSPO) has questioned the specific contribution of this protein in mediating the etifoxine neurosteroidogenic efficacy. Residence time (RT) at the binding site of the classic...

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Veröffentlicht in:	ACS chemical neuroscience 2017-07, Vol.8 (7), p.1448-1454
Hauptverfasser:	Costa, Barbara, Cavallini, Chiara, Da Pozzo, Eleonora, Taliani, Sabrina, Da Settimo, Federico, Martini, Claudia
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Anxiety Agents - metabolism Anti-Anxiety Agents - pharmacology Benzodiazepinones - metabolism Benzodiazepinones - pharmacology Binding Sites Binding, Competitive Carrier Proteins - metabolism Cell Line, Tumor Flumazenil - pharmacology GABA Modulators - pharmacology Hypolipidemic Agents - pharmacology Isoquinolines - pharmacology Kidney - drug effects Kidney - metabolism Kinetics Neurotransmitter Agents - metabolism Oxazines - metabolism Oxazines - pharmacokinetics Oxazines - pharmacology Pregnenolone - metabolism Radioligand Assay Rats Receptors, GABA-A - metabolism Thermodynamics Tritium
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