thiorphan

Thiorphan is a potent small molecule inhibitor of membrane metalloendopeptidase (enkephalinase, also known as neprilysin). It was the first synthetic enkephalinase inhibitor developed and displays antinociceptive activity after systemic administration. Thiorphan potentiates morphine-induced analgesia and attenuates naloxone-precipitated withdrawal symptoms. It also inhibits angiotensin-converting enzyme to a lesser extent. Thiorphan has been shown to reduce castor oil-induced diarrhea in animal models when administered intravenously but not intracerebroventricularly. In clinical use, thiorphan is the active metabolite of racecadotril (acetorphan), an antidiarrheal medication that acts by inhibiting enkephalinases in the gut to reduce pathological secretion without affecting gastrointestinal motility[1][2][4][5][6][7][10]. Experimental studies suggest neuroprotective effects against excitotoxic brain injury[8].

Other names

dl-thiorphan