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ANO1 is a potential analgesic target. DFBTA is a potent ANO1 inhibitor with excellent pharmacokinetics properties. In vivo PK were tested by Medicilon

2023-07-17

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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.

Reference:

Yuxi Wang, et al. Optimization of 4-arylthiophene-3-carboxylic acid derivatives as inhibitors of ANO1: Lead optimization studies toward their analgesic efficacy for inflammatory pain. Eur J Med Chem. 2022 Jul 5;237:114413. doi: 10.1016/j.ejmech.2022.114413.

non-steroidal anti-inflammatory analgesic-drug pharmacokinetics-properties oral-bioavailability

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