Synonyms: (S)-pregabalin | CI 1008 | Lyrica® | Nervalin® | PD 144723
pregabalin is an approved drug (FDA and EMA (2004))
Compound class:
Synthetic organic
Comment: Pregabalin is a gabapentinoid class anti-seizure medication. Chemically, it is a 3-isobutyl derivative of the inhibitory neurotransmitter γ-aminobutyric acid (GABA), but it appears to function as a modulator of voltage-gated calcium channels, rather than a GABA receptor agonist.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖View more information in the IUPHAR Pharmacology Education Project: pregabalin |
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References |
1. Hendrich J, Van Minh AT, Heblich F, Nieto-Rostro M, Watschinger K, Striessnig J, Wratten J, Davies A, Dolphin AC. (2008)
Pharmacological disruption of calcium channel trafficking by the alpha2delta ligand gabapentin. Proc Natl Acad Sci USA, 105 (9): 3628-33. [PMID:18299583] |
2. Schwarz JB, Colbry NL, Zhu Z, Nichelson B, Barta NS, Lin K, Hudack RA, Gibbons SE, Galatsis P, DeOrazio RJ et al.. (2006)
Carboxylate bioisosteres of pregabalin. Bioorg Med Chem Lett, 16 (13): 3559-63. [PMID:16621528] |
3. Schwarz JB, Gibbons SE, Graham SR, Colbry NL, Guzzo PR, Le VD, Vartanian MG, Kinsora JJ, Lotarski SM, Li Z et al.. (2005)
Novel cyclopropyl beta-amino acid analogues of pregabalin and gabapentin that target the alpha2-delta protein. J Med Chem, 48 (8): 3026-35. [PMID:15828841] |