R-phenibut binds to the α2–δ subunit of voltage-dependent calcium channels and exerts gabapentin-like anti-nociceptive effects

@article{Zvejniece2015RphenibutBT,
  title={R-phenibut binds to the $\alpha$2–$\delta$ subunit of voltage-dependent calcium channels and exerts gabapentin-like anti-nociceptive effects},
  author={Liga Zvejniece and Edijs Vāvers and Baiba Svalbe and Grigory Veinberg and Kristina Rizhanova and Vilnis Liepins and Ivars Kalvinsh and Maija Dambrova},
  journal={Pharmacology Biochemistry and Behavior},
  year={2015},
  volume={137},
  pages={23-29}
}
Phenibut is clinically used anxiolytic, mood elevator and nootropic drug. R-phenibut is responsible for the pharmacological activity of racemic phenibut, and this activity correlates with its binding affinity for GABAB receptors. In contrast, S-phenibut does not bind to GABAB receptors. In this study, we assessed the binding affinities of R-phenibut, S-phenibut, baclofen and gabapentin (GBP) for the α2-δ subunit of the voltage-dependent calcium channel (VDCC) using a subunit-selective ligand… Expand
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