Atagabalin Explained

Atagabalin (PD-0200,390) is a drug developed by Pfizer and related to gabapentin, which similarly binds to the α₂δ calcium channels (1 and 2).^[1] It was under development as a treatment for insomnia,^{[2] [3] [4]} but was discontinued following unsatisfactory trial results.

See also

• 4-Methylpregabalin
• Gabapentin enacarbil
• PD-217,014

Notes and References

1. Blakemore DC, Bryans JS, Carnell P, Carr CL, Chessum NE, Field MJ, Kinsella N, Osborne SA, Warren AN, Williams SC . Synthesis and in vivo evaluation of bicyclic gababutins . Bioorganic & Medicinal Chemistry Letters . 20 . 2 . 461–4 . January 2010 . 20005103 . 10.1016/j.bmcl.2009.11.118 .
2. Corrigan B, Feltner DE, Ouellet D, Werth JL, Moton AE, Gibson G . Effect of renal impairment on the pharmacokinetics of PD 0200390, a novel ligand for the voltage-gated calcium channel alpha-2-delta subunit . British Journal of Clinical Pharmacology . 68 . 2 . 174–80 . August 2009 . 19694735 . 2767279 . 10.1111/j.1365-2125.2009.03444.x .
3. Quintero JE, Pomerleau F, Huettl P, Johnson KW, Offord J, Gerhardt GA . Methodology for rapid measures of glutamate release in rat brain slices using ceramic-based microelectrode arrays: Basic characterization and drug pharmacology . Brain Research . 1401. 1–9. May 2011 . 21664606 . 10.1016/j.brainres.2011.05.025 . 3197737.
4. Kjellsson MC, Ouellet D, Corrigan B, Karlsson MO . Modeling Sleep Data for a New Drug in Development using Markov Mixed-Effects Models . Pharmaceutical Research . 28. 10. 2610–27. June 2011 . 21681607 . 10.1007/s11095-011-0490-x . 22241527 .