Discovery of aryl sulfonamide-selective Nav1.7 inhibitors with a highly hydrophobic ethanoanthracene core was written by Wang, Jin-tao;Zheng, Yue-ming;Chen, Yue-ting;Gu, Min;Gao, Zhao-bing;Nan, Fa-jun. And the article was included in Acta Pharmacologica Sinica in 2020.Recommanded Product: 111043-48-2 This article mentions the following:
Nav1.7 channels are mainly distributed in the peripheral nervous system. Blockade of Nav1.7 channels with small-mol. inhibitors in humans might provide pain relief without affecting the central nervous system. Based on the facts that many reported Nav1.7-selective inhibitors contain aryl sulfonamide fragments, as well as a tricyclic antidepressant, maprotiline, has been found to inhibit Nav1.7 channels, we designed and synthesized a series of compounds with ethanoanthracene and aryl sulfonamide moieties. Their inhibitory activity on sodium channels were detected with electrophysiol. techniques. We found that compound 10o potently inhibited Nav1.7 channels stably expressed in HEK293 cells (IC50 = 0.64 ± 0.30 nmol/L) and displayed a high Nav1.7/Nav1.5 selectivity. In mouse small-sized dorsal root ganglion neurons, compound 10o (10, 100 nmol/L) dose-dependently decreased the sodium currents and dramatically suppressed depolarizing current-elicited neuronal discharge. Preliminary in vivo experiments showed that compound 10o possessed good analgesic activity: in a mouse visceral pain model, administration of compound 10o (30-100 mg/kg, i.p.) effectively and dose-dependently suppressed acetic acid-induced writhing. In the experiment, the researchers used many compounds, for example, 3-Hydroxy-1-methylazetidine (cas: 111043-48-2Recommanded Product: 111043-48-2).
3-Hydroxy-1-methylazetidine (cas: 111043-48-2) belongs to alcohols. Alcohols are among the most common organic compounds. They are used as sweeteners and in making perfumes, are valuable intermediates in the synthesis of other compounds, and are among the most abundantly produced organic chemicals in industry. A multistep synthesis may use Grignard-like reactions to form an alcohol with the desired carbon structure, followed by reactions to convert the hydroxyl group of the alcohol to the desired functionality.Recommanded Product: 111043-48-2
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts