ABSTRACT
Anoctamin 1 (ANO1) is a kind of calcium-activated chloride channel involved in nerve depolarization. ANO1 inhibitors display significant analgesic activity by the local peripheral and intrathecal administration. In this study, several thiophenecarboxylic acid and benzoic acid derivatives were identified as novel ANO1 inhibitors through the shape-based virtual screening, among which the 4-arylthiophene-3-carboxylic acid analogues with the best ANO1 inhibitory activity were designed, synthesized and compound
ABSTRACT
Objective To observe the role of community popular opinion leader (POL) intervention on ocular epidemic study. Methods During the process of epidemiological survey of eye disease in Shenyang City,the community POL was interviewed to observe the change of the follow-up population from 2015 to 2016 and the effects of the POL intervention were analyzed. Results The study population follow-up rate was significantly improved after POL intervention (χ2 = 85.42,P < 0.01),the male-to-female ratio was balanced (χ2 = 6.51, P = 0.01),and more participants were willing and hoped to participate in the epidemic study for a long time. Conclusion Community POLs can improve the follow-up rate of epidemiological surveys and mobilize the enthusiasm of the population to participate in epidemiological investigations.
ABSTRACT
To explore novel non-opioid analgesic agents, 16 compounds were synthesized and their structures were confirmed by 1H NMR and HR-MS. YX0611-1 was treated as the leading compound. The results of mice writhing model and hot plate model showed that compounds 2, 7, 8, 9, 11 and 15 had obvious analgesic activities in vivo. The test of affinity to mu, delta, kappa receptor displayed that active compounds didn't act on opioid receptor. The results of preliminary toxicity and pharmacokinetic tests showed that compound 7 had better safety and pharmacokinetic properties than that of YX0611-1, and it deserved further development.