Recently I am researching about VITRO PHARMACOLOGICAL CHARACTERIZATION; RELEASE; AGONIST; SCHIZOPHRENIA; DISCOVERY; TARGETS; SERIES; ACID, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [NSFC 21572011, 81573410, 31370741, 21272009]; Ministry of Science and Technology of ChinaMinistry of Science and Technology, China [2013CB531302]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: 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. The CAS is 87-63-8. Through research, I have a further understanding and discovery of 2-Chloro-6-methylaniline. Quality Control of 2-Chloro-6-methylaniline
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
About 2-Chloro-6-methylaniline, 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 concate me.. Quality Control of 2-Chloro-6-methylaniline
Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics