TROX-1 explained

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]

Notes and References

  1. Abbadie C, McManus OB, Sun SY, Bugianesi RM, Dai G, Haedo RJ, Herrington JB, Kaczorowski GJ, Smith MM, Swensen AM, Warren VA, Williams B, Arneric SP, Eduljee C, Snutch TP, Tringham EW, Jochnowitz N, Liang A, Euan MacIntyre D, McGowan E, Mistry S, White VV, Hoyt SB, London C, Lyons KA, Bunting PB, Volksdorf S, Duffy JL . 6 . 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 . August 2010 . 20439438 . 10.1124/jpet.110.166363 . 25588800 .
  2. Swensen AM, Herrington J, Bugianesi RM, Dai G, Haedo RJ, Ratliff KS, Smith MM, Warren VA, Arneric SP, Eduljee C, Parker D, Snutch TP, Hoyt SB, London C, Duffy JL, Kaczorowski GJ, McManus OB . 6 . 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 . March 2012 . 22188924 . 10.1124/mol.111.075226 . 1617039 .
  3. Rahman W, Patel R, Dickenson AH . 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 . October 2015 . 26247695 . 4564012 . 10.1016/j.neuroscience.2015.07.073 .

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