PD-217,014

Chemical compound
PD-217,014
Identifiers
  • (1α,3α,5α)-3-aminomethyl-bicyclo[3.2.0]heptane-3-acetic acid
CAS Number
  • 444088-20-4 checkY
PubChem CID
  • 10313401
ChemSpider
  • 19264101
UNII
  • K2T93E812G
Chemical and physical data
FormulaC10H17NO2
Molar mass183.251 g·mol−1
3D model (JSmol)
  • Interactive image
  • C1C[C@@H]2[C@H]1C[C@](C2)(CC(=O)O)CN
InChI
  • InChI=1S/C10H17NO2/c11-6-10(5-9(12)13)3-7-1-2-8(7)4-10/h7-8H,1-6,11H2,(H,12,13)/t7-,8+,10+
  • Key:NDDZVQRQVFTNSN-MBTKJCJQSA-N

PD-217,014 is a drug developed by Pfizer and related to gabapentin, which similarly binds to the α2δ calcium channels (1 and 2). It was developed as a potentially more potent successor to gabapentin and pregabalin, along with several other analogues such as atagabalin and 4-methylpregabalin, but while PD-217,014 produces visceral analgesic effects in animal studies with higher potency and efficacy than gabapentin, it was not developed further for clinical use because of its comparatively more complex synthesis, compared to other related analogues.[1]

References

  1. ^ Ohashi K, Kawai M, Ninomiya N, Taylor C, Kurebayashi Y (2008). "Effect of a new alpha 2 delta ligand PD-217014 on visceral hypersensitivity induced by 2,4,6-trinitrobenzene sulfonic acid in rats". Pharmacology. 81 (2): 144–50. doi:10.1159/000110737. PMID 17989503. S2CID 84708161.
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Analgesics (N02A, N02B)
Opioids
Opiates/opium
Semisynthetic
Synthetic
Paracetamol-typeNSAIDs
Propionates
Oxicams
Acetates
COX-2 inhibitors
Fenamates
Salicylates
Pyrazolones
Others
CannabinoidsIon channel
modulators
Calcium blockers
Sodium blockers
Potassium openers
MyorelaxantsOthers
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Calcium
VDCCsTooltip Voltage-dependent calcium channels
Blockers
Activators
Potassium
VGKCsTooltip Voltage-gated potassium channels
Blockers
Activators
IRKsTooltip Inwardly rectifying potassium channel
Blockers
Activators
  • GIRKTooltip G protein-coupled inwardly rectifying potassium channel-specific: ML-297 (VU0456810)
KCaTooltip Calcium-activated potassium channel
Blockers
  • BKCa-specific: Ethanol (alcohol)
  • GAL-021
Activators
K2PsTooltip Tandem pore domain potassium channel
Blockers
Activators
Sodium
VGSCsTooltip Voltage-gated sodium channels
Blockers
Activators
ENaCTooltip Epithelial sodium channel
Blockers
Activators
  • Solnatide
ASICsTooltip Acid-sensing ion channel
Blockers
Chloride
CaCCsTooltip Calcium-activated chloride channel
Blockers
Activators
CFTRTooltip Cystic fibrosis transmembrane conductance regulator
Blockers
Activators
Unsorted
Blockers
Others
TRPsTooltip Transient receptor potential channels
  • See here instead.
LGICsTooltip Ligand gated ion channels
  • See here instead.
See also: Receptor/signaling modulators • Transient receptor potential channel modulators


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