A-836339 is a potent and selective CB(2) agonist. A-836339 displays high affinities at CB(2) receptors and selectivity over CB(1) receptors in both human and rat. In addition A-836339 exhibits a profile devoid of significant affinity at other G-protein-coupled receptors and ion channels. A-836339 has also demonstrated efficacies in the chronic constrain injury (CCI) model of neuropathic pain, skin incision, and capsaicin-induced secondary mechanical hyperalgesia models[3]. Systemic administration of A-836339 (0.3-3 micromol/kg, i.v.) reduced both evoked and spontaneous WDR (wide dynamic range) neuronal activity in neuropathic, but not sham rats. Similar to systemic delivery, intra-spinal injection of A-836339 (0.3 and 1 nmol) also attenuated both von Frey-evoked and spontaneous firing of WDR neurons in neuropathic rats. Application of A-836339 (3-30 nmol) onto the ipsilateral L5 dorsal root ganglion (DRG) of neuropathic rats reduced the von Frey-evoked activity of WDR neurons, but spontaneous firing was unaltered[4].
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