Li, Yuanheng; Sun, Lilan; Yang, Taoyi; Jiao, Wenxuan; Tang, Jingshu; Huang, Xiaomin; Huang, Zongze; Meng, Ying; Luo, Laichun; Wang, Xintong; Bian, Xiling; Zhang, Fang; Wang, KeWei; Sun, Qi published the artcile< Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice>, Application of C7H8ClN, the main research area is thiazolo pyrimidinone preparation nicotinic acetylcholine receptor allosteric modulator SAR.
A series of novel thiazolo[4,5-d]pyrimidin-7(6H)-ones were designed, synthesized, and evaluated as the type I pos. allosteric modulators of human α7 nAChR expressed in Xenopus oocytes by a two-electrode voltage clamp. The structure-activity relationship anal. identified the compound I as a potent and efficacious PAM with the maximum activation effect of the α7 current of over 1633% in the presence of acetylcholine (100 μM) and an EC50 = 1.26 μM. It is highly specific to α7 nAChR over other subtypes of nAChR, 5-HT3A, NMDA, and GABAA receptors. Compound I 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 I dose-dependently (0.1-1 mg/kg, i.p.) reversed the prepulse inhibition deficit induced by MK-801 in the mouse schizophrenia model.
Journal of Medicinal Chemistry published new progress about 5-HT3A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 29027-20-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H8ClN, Application of C7H8ClN.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics