repinotan

Repinotan is a small molecule drug developed as a highly selective, high-affinity full agonist of the serotonin 5-HT1A receptor. It is an aminomethylchroman derivative with neuroprotective properties demonstrated in animal models and investigated in humans for acute ischemic stroke and traumatic brain injury. Repinotan acts primarily by activating pre- and post-synaptic 5-HT1A receptors, leading to neuronal hyperpolarization via G protein-coupled inwardly rectifying potassium channels. This results in inhibition of neuron firing and reduced glutamate release, protecting neurons from overexcitation. Additional mechanisms include activation of anti-apoptotic pathways (such as PI3K), increased expression of Bcl-2, inhibition of caspase-3 activity through MAPK and PKCα signaling, modulation of glial growth factor S-100β, and nerve growth factor levels. Repinotan was developed by Bayer for potential use in treating acute ischemic stroke and traumatic brain injury but did not progress beyond Phase II clinical trials[1][4][5][6].

Other names

repinotan hydrochloride