TROX-1

Chemical compound
TROX-1
Identifiers
  • (3R)-5-(3-chloro-4-fluorophenyl)-3-methyl-3-(pyrimidin-5-ylmethyl)-1-(1H-1,2,4-triazol-3-yl)-1,3-dihydro-2H-indol-2-one
CAS Number
  • 1141080-15-0
PubChem CID
  • 25256198
ChemSpider
  • 24750794
UNII
  • GWS86V23Q8
CompTox Dashboard (EPA)
  • DTXSID40649497 Edit this at Wikidata
Chemical and physical data
FormulaC22H16ClFN6O
Molar mass434.86 g·mol−1
3D model (JSmol)
  • Interactive image
  • C[C@]5(Cc1cncnc1)C(=O)N(c2nc[nH]n2)c4ccc(c3ccc(F)c(Cl)c3)cc45

TROX-1 is a drug which acts as a potent blocker of the Cav2 type calcium channels. It was developed as a potential analgesic after the discovery that the selective Cav2.2 blocker ziconotide is an active analgesic with similar efficacy to strong opioid drugs. Unlike ziconotide, TROX-1 is not so selective, and also blocks the Cav2.1 and Cav2.3 calcium channel subtypes, but it has the great advantage of being orally active, whereas ziconotide must be administered intrathecally, by injection into the spinal fluid. In animal studies of TROX-1, analgesic effects were observed with similar efficacy to NSAIDs such as naproxen or diclofenac, and anti-allodynia effects equivalent to pregabalin or duloxetine.[1][2][3]

References

  1. ^ Abbadie C, McManus OB, Sun SY, Bugianesi RM, Dai G, Haedo RJ, et al. (August 2010). "Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker". The Journal of Pharmacology and Experimental Therapeutics. 334 (2): 545–55. doi:10.1124/jpet.110.166363. PMID 20439438. S2CID 25588800.
  2. ^ Swensen AM, Herrington J, Bugianesi RM, Dai G, Haedo RJ, Ratliff KS, et al. (March 2012). "Characterization of the substituted N-triazole oxindole TROX-1, a small-molecule, state-dependent inhibitor of Ca(V)2 calcium channels". Molecular Pharmacology. 81 (3): 488–97. doi:10.1124/mol.111.075226. PMID 22188924. S2CID 1617039.
  3. ^ Rahman W, Patel R, Dickenson AH (October 2015). "Electrophysiological evidence for voltage-gated calcium channel 2 (Cav2) modulation of mechano- and thermosensitive spinal neuronal responses in a rat model of osteoarthritis". Neuroscience. 305: 76–85. doi:10.1016/j.neuroscience.2015.07.073. PMC 4564012. PMID 26247695.
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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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