Chemistry:TROX-1
From HandWiki
Short description: Chemical compound
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| Formula | C22H16ClFN6O |
| Molar mass | 434.86 g·mol−1 |
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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
- ↑ "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. doi:10.1124/jpet.110.166363. PMID 20439438.
- ↑ "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. doi:10.1124/mol.111.075226. PMID 22188924.
- ↑ "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. doi:10.1016/j.neuroscience.2015.07.073. PMID 26247695.
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