Selective neurokinin-1 receptor antagonists are anti-hyperalgesic in a model of neuropathic pain in the guinea-pig

作者: E.A Campbell , C.T Gentry , S Patel , M.S Panesar , C.S.J Walpole

DOI: 10.1016/S0306-4522(98)00318-2

关键词: AnesthesiaNeuralgiaAntagonistHyperalgesiaGuinea pigPharmacologyReceptorPeripheral neuropathyAnalgesicMedicineNeuropathic pain

摘要: Neuropathic pain is poorly managed by conventional analgesic therapy, such as non-steroidal anti-inflammatory drugs and opiates. The development of animal models peripheral neural damage has aided in our understanding the pathology pharmacology neuropathic pain. This report first clear demonstration using selective neurokinin-1 receptor antagonists a potentially novel therapeutic approach to treatment resulting from nerve guinea-pig model. antagonists, SDZ NKT 343 LY 303,870 significantly reduced mechanical hyperalgesia following oral intrathecal administration. (R,R)-SDZ NK T343, enantiomer did not show anti-hyperalgesic activity. RPR 100,893 showed significant activity only administration suggesting poor absorption or low level penetration blood-brain barrier. These results imply that offer new class with largely central site action

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