2016年5月31日 · Here, we show that chronic administration of the orally bioavailable mGluR5-selective negative allosteric modulator CTEP, which is similar in structure, potency, and selectivity to Basimglurant (RO4917523), which is currently in phase II clinical development for major depressive disorder and fragile X syndrome, reverses cognitive decline in ...

2021年9月29日 · Here we confirm that FXS model mice display acquired treatment resistance after chronic treatment with the mGluR5 NAM CTEP in three assays commonly examined in the mouse model of FXS: (1) audiogenic seizure susceptibility, (2) sensory cortex hyperexcitability, and (3) hippocampal protein synthesis.

2021年9月28日 · The mGluR5 specific negative allosteric modulator CTEP (chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine) was purchased from Sigma-Aldrich (SML2306) and administered at 2 mg/kg …

CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.

Potential pharmacotherapies such as mGluR5 inhibitors (e.g. CTEP; 2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazole-4-yl)ethynyl)pyridine), GABA B R agonists (e.g. arbaclofen) and δ-containing GABA A R agonists (e.g. gaboxadol) have not translated into clinical success despite rescuing many phenotypes in the Fmr1-KO model ...

2016年5月31日 · Here, we show that chronic administration of the orally bioavailable mGluR5-selective negative allosteric modulator CTEP, which is similar in structure, potency, and selectivity to Basimglurant (RO4917523), which is currently in phase II clinical development for major depressive disorder and fragile X syndrome, reverses cognitive decline in ...

Here, we show that chronic admin-istration of the orally bioavailable mGluR5-selective negative allosteric modulator CTEP, which is similar in structure, potency, and selectivity to Basimglur-ant (RO4917523), which is currently in phase II clin-ical development for major depressive disorder and fragile X syndrome, reverses cognitive decline in A...

CTEP (RO4956371, RO 4956371, mGluR5 inhibitor)是可口服的mGlu5受体选择性变构调节剂，IC 50 为2.2 nM，具有反向激动剂的活性。代谢型谷氨酸受体5 (mGlu5 Receptor)是一种谷氨酸激活的CG类蛋白偶联受体，在中枢神经系统中广泛表达，并作为一系列适应症的药物靶点进行临床研究 ...

2022年2月2日 · Here, we investigated whether targeted antagonism of mGluR5 using CTEP differentially improves HD symptoms and neuropathology in male versus female zQ175 HD mice. We find indeed that chronic treatment with CTEP differentially improves motor and cognitive deficits in male and female zQ175 mice.

Potent, orally bioavailable, long lasting and selective mGluR5 allosteric antagonist or negative allosteric modulator; CTEP binds mGluR5 with low nanomolar affinity and shows >1000-fold selectivity against other targets, including all known mGlu receptorsCTEP has considerably improved properties over older mGluR5 antagonists such as MPEP and ...