In vitro Efficacy as Determined by Radioligand Transporter Assays Using Recombinant Human Monoamine Transporter Proteins. pIC50 Denotes the Negative Decadic Logarithm of the Half-Maximum Effect Concentration [M].
In vitro Pharmacological Profile of (R)-Sila-venlafaxine
(R)-Sila-venlafaxine is a selective noradrenaline reuptake inhibitor.
In vitro tests across a panel of 68 common receptors/channels and 16 enzymes:
(R)-Sila-venlafaxine is inactive in all assays (< 50% inhibition at 10 µM) except for weak affinity at Ca2+ and Na+ channels.
Evaluation of (R)-Sila-venlafaxine in a Ferret Model of Morphine-Induced Emesis
(R)-Sila-venlafaxine was dosed orally in ferrets 2 h prior to the emetogen (morphine, 0.125 mg/kg, s.c.; group size, n = 4). The ferrets were monitored for emetic episodes (retching and vomiting events) for 2 h following the administration of morphine.
At 50 mg/kg (R)-sila-venlafaxine completely abolishes emetic episodes, and almost complete inhibition (93%) is achieved at 5 mg/kg.
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J. B. Warneck, F. H. M. Cheng, M. J. Barnes, J. S. Mills, J. G. Montana, R. J. Naylor, M.-P. Ngan, M.-K. Wai, J. O. Daiss, R. Tacke, J. A. Rudd, Toxicology and Applied Pharmacology, 2008, in press.