translocator protein

Chlormezanone (Trancopal) is a non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.

Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. GABAA receptor Etifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration. Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons.

DPA-714 is a high-affinity translocator protein (TSPO) ligand (Ki=7 nM) designed with a fluorine atom, allowing labeling with fluorine-18 for in vivo imaging via positron emission tomography. [18F]DPA-714 successfully enables specific imaging of inflammation in various neuroinflammation models and a brain tumor model.

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

Desalkylgidazepam, a benzodiazepine compound, is a metabolite of gidazepam. It is capable of activating both GABA A-type receptors and the translocator protein (TSPO).

TSPO Carbonic Anhydrase Modulator 1 (Compound 3) acts as a dual modulator of mitochondrial translocator protein and carbonic anhydrase, with a TSPOKi of 1.340 μM and a CAVII KA of 10.7 μM. It enhances neurosteroid production, increases BDNF gene expression, and demonstrates neuroprotective activity.

high affinity agonist of the translocator protein

Emapunil (XBD-173) is an anxiolytic drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO.

ER176 is a novel PET radioligand utilized for the visualization of 18 kDa translocator protein (TSPO), a neuroinflammation biomarker, marking the advancement in imaging technology.

TSPO Ligand-Linker Conjugates 1, comprising a translocator protein (TSPO) ligand and a linker, is instrumental in synthesizing mitochondria-targeting autophagy-targeting chimera (AUTAC). This compound binds TSPO on the outer mitochondrial membrane (OMM), facilitating the degradation of malfunctioning mitochondria and proteins through mitophagy, thereby enhancing mitochondrial function. It holds potential applications in research related to mitochondrial dysfunction, encompassing neurodegenerative diseases, cancer, and diabetes [1].