An article Design and Synthesis of Novel Positive Allosteric Modulators of alpha 7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice WOS:000455561400010 published article about VITRO PHARMACOLOGICAL CHARACTERIZATION; RELEASE; AGONIST; SCHIZOPHRENIA; DISCOVERY; TARGETS; SERIES; ACID in [Li, Yuanheng; Jiao, Wenxuan; Huang, Zongze; Meng, Ying; Luo, Laichun; Wang, KeWei; Sun, Qi] Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China; [Sun, Lilan; Zhang, Fang; Wang, KeWei] Qingdao Univ, Sch Pharm, Dept Pharmacol, Qingdao 266021, Peoples R China; [Yang, Taoyi; Tang, Jingshu; Huang, Xiaomin; Wang, Xintong; Bian, Xiling; Wang, KeWei] Peking Univ, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100191, Peoples R China in 2019, Cited 49. Application In Synthesis of 2-Chloro-6-methylaniline. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8
A series of novel thiazolo[4,5-d]pyrimidin-7(6H)-ones (3aa-3eq) were designed, synthesized, and evaluated as the type I positive allosteric modulators of human alpha 7 nAChR expressed in Xenopus ooctyes by a two-electrode voltage clamp. The structure-activity relationship analysis identified the compound 3ea as a potent and efficacious PAM with the maximum activation effect of the alpha 7 current of over 1633% in the presence of acetylcholine (100 mu M) and an EC50 = 1.26 mu M. It is highly specific to alpha 7 nAChR over other subtypes of nAChR, 5-HT3A, NMDA, and GABA(A) receptors. Compound 3ea showed an elimination half-life of 10.8 +/- 1.5 h for 3 mg/kg, i.v., and 7.4 +/- 1.1 h for 60 mg/kg, i.g. in rat. It also exhibited sufficient blood-brain barrier penetration with no significant effect on hERG channel. Most importantly, compound 3ea dose-dependently (0.1-1 mg/kg, i.p.) reversed the prepulse inhibition deficit induced by MK-801 in the mouse schizophrenia model. X
Application In Synthesis of 2-Chloro-6-methylaniline. Welcome to talk about 87-63-8, If you have any questions, you can contact Li, YH; Sun, LL; Yang, TY; Jiao, WX; Tang, JS; Huang, XM; Huang, ZZ; Meng, Y; Luo, LC; Wang, XT; Bian, XL; Zhang, F; Wang, KW; Sun, Q or send Email.
Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
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