rat and human tspo

ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels, and enzymes. ONO-2952 is a potent and selective translocator protein 18 kDa (TSPO) antagonist (Ki: 0.33-9.30 nM for rat and human TSPO). ONO-2952 has the potential for i

Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active activator of Kv7.2/Kv7.3 channels and the TSPO. It activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). This compound protects motor neurons from degeneration caused by exposure to astrocyte-conditioned media from mice and humans with amyotrophic lateral sclerosis/frontotemporal dementia. Additionally, Kv7.2/Kv7.3 activator-3 stimulates axonal growth in dorsal root ganglia through TSPO and Kv7.2/3 activation and exhibits anticonvulsant effects in epilepsy models. It alleviates hyperalgesia in diabetic neuropathy patients, enhances the survival and regeneration of neurons after cervical neuropathy in rats, and accelerates the recovery of normal function in sensory and motor neurons.

(R)-ONO-2952 is the R-enantiomer of ONO-2952. ONO-2952 is selective and oral effective TSPO antagonist, with Kis of 0.330-9.30 nM inhibiting rat and human TSPO.