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ANO1是一个潜在的镇痛靶点。DFBTA是一种有效的ANO1抑制剂,具有优异的药代动力学特性。体内PK测试通过beats365进行

2023-07-06
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Current pain management is largely limited to opioids and non-steroidal anti-inflammatory drugs. Developing new analgesic drugs remains important to address the unmet medical needs of chronic pain patients. Calcium-activated chloride channel anoctamin-1 (ANO1) is a potential analgesic target. DFBTA is a potent inhibitor with the IC50 of 24 nM. DFBTA shows very weak cytotoxicity, cardiotoxicity, and acute toxicity, as well as excellent pharmacokinetics properties with oral bioavailability >75% and little brain penetration (<1.5% brain/plasma). In vivo PK were tested by Medicilon

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