crobenetine

Crobenetine is a small molecule benzomorphan derivative developed by Boehringer Ingelheim. It acts as a use-dependent sodium channel blocker—specifically antagonizing the sodium channel protein type II alpha subunit (Nav1.2). Crobenetine displaces radioligand from neurotoxin receptor site 2 of the Na(+) channel in rat brain synaptosomes with high potency (IC50 ~49 nM), showing greater affinity for inactivated channels than resting ones. In preclinical models it demonstrated neuroprotective effects after focal cerebral ischemia and produced significant analgesic and anti-hyperalgesic effects in animal models of pain and arthritis. Crobenetine was investigated up to phase 2 clinical trials for acute ischemic stroke and pain but development was discontinued before approval[1][2][4].

Other names

crobenetine hydrochloride(2R,6S)-3-[2(S)-Benzyloxypropyl]-6,11,11-trimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-10-ol