Related Products of 123536-14-1, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a article£¬once mentioned of 123536-14-1
Discovery of fused heterocyclic carboxamide derivatives as novel alpha7-nAChR agonists: Synthesis, preliminary SAR and biological evaluation
The alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) has emerged as a promising therapeutic target for schizophrenia. In our previous work, a novel series of alpha7-nAChR agonists bearing scaffold of indolizine were discovered. To explore the effect of aromaticity on the activity and find more active agents, herein, fused heterocyclic carboxamide derivatives were designed and synthesized in this study. Based on the evaluation by two-electrode voltage clamp in Xenopus oocytes, 27 of the synthesized compounds showed obvious agonism of alpha7 nAChR. Particularly, compounds 10a and 10e showed significantly higher Emax than EVP-6124. The result illustrated the importance of aromaticity to the activity of agonism. Compound 10a, which showed EC50 of 1.88 muM and Emax of 72.4%, was further characterized comprehensively, including co-application with type II positive allosteric modulator PNU-120596, selectivity with other closely related ligand-gated ion channel, etc. The results showed that 10a showed moderate selectivity over other subtypes such as alpha4beta2 and alpha3beta4 nAChR. 10a evoked alpha7-like currents that were inhibited by MLA and enhanced in the presence of the alpha7 PAM PNU-120596. The analysis of binding mode and understanding of structure-activity relationship provided insights to develop more potent novel alpha7-nAChR agonists.
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Quinuclidine – Wikipedia,
Quinuclidine | C7H158N | ChemSpider