生物活性

• 描述CTEP is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC₅₀ of 2.2 nM. CTEP binds mGlu5 with low nanomolar affinity and shows > 1000-fold selectivity over other mGlu receptors. In vivo, CTEP is active in the stress-induced hyperthermia procedure in mice and the Vogel conflict drinking test in rats with minimal effective doses of 0.1 and 0.3 mg/kg. In vitro, CTEP inhibits the constitutive activity of human mGlu5 by approximately 50% with an IC₅₀ of 40.1 nM in HEK293 cells stably expressing human mGlu5^[3].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00903968	Multiple Myeloma	Phase 1 Phase 2	Completed	-	United States, Massachusetts ... more >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 Cape Cod Hospital Hyannis, Massachusetts, United States, 02601 Milford Hospital Milford, Massachusetts, United States, 01757 Newton-Wellesley Hospital Newton, Massachusetts, United States, 02462 United States, Pennsylvania Cancer Treatment Centers of America (Eastern Regional Medical Center) Philadelphia, Pennsylvania, United States, 19124 Collapse <<
  NCT00903968	-	-	Completed	-	-
  NCT03370276	Squamous Cell Carcinoma of the... more >> Oropharynx Squamous Cell Carcinoma of the Larynx Squamous Cell Carcinoma of the Oral Cavity Squamous Cell Carcinoma of the Hypopharynx Squamous Cell Carcinoma of the Paranasal Sinus Head and Neck Squamous Cell Carcinoma Squamous Cell Cancer Head and Neck Carcinoma Collapse <<	Phase 1 Phase 2	Recruiting	December 2022	United States, Florida ... more >> H. Lee Moffitt Cancer Center and Research Institute Recruiting Tampa, Florida, United States, 33612 Contact: Matthew Johnson    813-745-5434    matthew.johnson@moffitt.org    Principal Investigator: Christine H. Chung, M.D.          Sub-Investigator: Julie Kish, M.D.          Sub-Investigator: Jameel Muzaffar, M.D.          United States, Georgia Emory University School of Medicine Not yet recruiting Atlanta, Georgia, United States, 30322 Contact: Nabil Saba, M.D.    404-778-3126    nfsaba@emory.edu    Sub-Investigator: Nabil Saba, M.D.          United States, Ohio The Ohio State University Not yet recruiting Columbus, Ohio, United States, 43210 Contact: James Rocco, M.D., Ph.D.    614-293-8074    James.Rocco@osumc.edu    Sub-Investigator: James Rocco, M.D., Ph.D. Collapse <<

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• 参考文献

• [1] Michalon A, Sidorov M, et al. Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice. Neuron. 2012 Apr 12;74(1):49-56.

  [2] Lindemann L, Jaeschke G, et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86.

  [3] Lindemann L, Jaeschke G, Michalon A, Vieira E, Honer M, Spooren W, Porter R, Hartung T, Kolczewski S, Büttelmann B, Flament C, Diener C, Fischer C, Gatti S, Prinssen EP, Parrott N, Hoffmann G, Wettstein JG. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86. doi: 10.1124/jpet.111.185660. Epub 2011 Aug 17. PMID: 21849627.