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- W2333744463 abstract "GLYX-13 is an amidated tetrapeptide (Thre-Pro-Pro-Thre-NH2) that has been shown to be a robust cognitive enhancer and antidepressant. Currently GLYX-13 is entering Phase III clinical trials for major depressive disorder. GLYX-13 was evaluated in two rat surgical models of the neuropathic pain: Chung (spinal nerve ligation) and Bennett (chronic nerve constriction). Pain responses were measured using Von Frey filaments and the Dixon up-down method. At its optimal dose level (5mg/kg, IV), GLYX-13 produced a robust analgesic effect (compared to saline vehicle) in these models 1 hr, 24 hr and 1 week following a single dose without any adverse effects. In comparison, the analgesic effect of a single dose of gabapentin (150 mg/kg PO) was present at 1 hr but not 24 hr. Previously, it was shown that GLYX-13 (5 mg/kg IV) produces an analgesic effect in the late phase of the rat formalin model of neuropathic pain. Since the site of action of NMDA receptor modulators as analgesics has been controversial, medial prefrontal cortex (prelimbic or infralimbic) injections of GLYX-13 (0.1, 1, or 10 μg/side) were also performed. GLYX-13 produced an analgesic effect in the late phase of the rat formalin model (compared to saline vehicle) for up to 1 month following a single dose as measured as weighted pain score. This effect was not observed following injections of GLYX-13 (1 μg/side) into the primary / secondary motor cortex. As expected, GLYX-13 did not produce any effect when evaluated in two rat nociceptive pain models (carrageenan and tail flick). GLYX-13 did not alter locomotor activity in the open field or produce ataxia in the rotarod test across a wide dose range, and shows a therapeutic index of > 100. These data show that GLYX-13 has therapeutic potential for the treatment of neuropathic pain." @default.
- W2333744463 created "2016-06-24" @default.
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- W2333744463 date "2015-04-01" @default.
- W2333744463 modified "2023-09-23" @default.
- W2333744463 title "(278) GLYX-13, an N-methyl-D-aspartate functional glycine site partial agonist, is efficacious in rat surgical models of neuropathic pain" @default.
- W2333744463 doi "https://doi.org/10.1016/j.jpain.2015.01.196" @default.
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