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Tiaprenorphine is a small molecule opioid receptor modulator developed by Beijing Ziduhongye Technology Development for the treatment of opioid use disorder. As a derivative of buprenorphine, it functions as a partial agonist at the mu-opioid receptor (MOR) and an antagonist at the kappa-opioid receptor (KOR). This pharmacological profile is designed to reduce opioid cravings and prevent relapse while minimizing the risk of respiratory depression and physical dependence compared to full mu-opioid agonists. It has been evaluated in clinical trials in China for relapse prevention following detoxification in opioid-dependent patients, specifically focusing on maintaining abstinence and improving tolerability compared to traditional maintenance therapies.
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