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Rapastinel (INN) (code name GLYX-13) is an intravenously-administered, selective, weak partial agonist of the glycine site of the NMDA receptor (IA ≈ 25%) which is under development by Naurex as an adjunctive therapy for treatment-resistant depression. It is an amidated tetrapeptide (Thr-Pro-Pro-Thr-NH2) which rapidly crosses the blood-brain-barrier, but is not active orally.〔http://webcache.googleusercontent.com/search?q=cache:I8h0z6_2oscJ:adisinsight.springer.com/drugs/800031281+&cd=2&hl=en&ct=clnk&gl=us〕 On March 3, 2014 the FDA granted Fast Track designation to the development of rapastinel as an adjunctive therapy in treatment-resistant major depressive disorder.〔FDA Grants Fast Track Designation to Naurex's Rapid-Acting Novel Antidepressant GLYX-13 http://www.prnewswire.com/news-releases/fda-grants-fast-track-designation-to-naurexs-rapid-acting-novel-antidepressant-glyx-13-248174561.html〕 As of 2015, the drug has completed phase II clinical development for this indication.〔http://naurex.com/wp-content/uploads/2014/12/Naurex_P2b_Data_Press_Release_FINAL_Approved.pdf〕 Phase III clinical trials will be starting in 2015.〔 In addition to its antidepressant effects, rapastinel has been shown to enhance memory and learning in both young adult and learning-impaired, aging rat models. It has been shown to increase Schaffer collateral-CA1 long-term potentiation ''in vitro''. In concert with a learning task, rapastinel has also been shown to elevate gene expression of hippocampal NR1, a subunit of the NMDA receptor, in 3-month-old rats. Neuroprotective effects have also been demonstrated in Mongolian Gerbils by delaying the death of CA1, CA3, and dentate gyrus pyramidal neurons under glucose and oxygen-deprived conditions. Additionally, rapastinel has demonstrated antinociceptive activity, which is of particular interest, as both competitive and noncompetitive NMDA receptor antagonists are ataxic at analgesic doses, while rapastinel and other glycine subunit ligands are able to elicit analgesia at sub-ataxic doses. ==See also== * ALKS-5461 * AV-101 * CERC-301 * Esketamine * Nebostinel * NRX-1074 * NSI-189 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「rapastinel」の詳細全文を読む スポンサード リンク
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