Atagabalin, also known as PD 0200390, is a gabamimetic agent under development for the treatment for insomnia. Atagabalin is related to gabapentin, which similarly binds to the α2δ calciumchannels (1 and 2). It was discontinued following unsatisfactory t
Mirogabalin besylate is a potent and orally active ligand that selectively targets the α2δ subunit of voltage-gated calciumchannels. It displays high affinity (K d ) values, namely 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM, for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.