A-889425 is a selective and competitive TRPV1 channel blocker with an IC50 of 335 nM to displace capsaicin at rat receptors, and has good penetration into the CNS. In the somatic sensory system, receptor-selective TRPV1 antagonists, such as A-889425 attenuate mechanical hyperalgesia in models of inflammatory, osteoarthritic, and neuropathic pain. Administration of A-889425 inhibited mechanically evoked activity of wide dynamic range (WDR) neurons in the rat spinal dorsal horn under conditions of peripheral inflammation but not in uninjured rats1. In addition to actions on the nociceptive system, several TRPV1 blockers like A-889425 have been reported to also affect thermoregulation by transiently raising core body temperature following systemic administration in both animals and humans.
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