View source for TROX-1

{{Short description|Chemical compound}}
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{{Drugbox
| IUPAC_name = (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
| image = TROX-1_structure.png
| width = 220
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| pregnancy_US = <!-- A / B            / C / D / X -->
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 -->
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<!--Identifiers-->
| CAS_number = 1141080-15-0
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| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = GWS86V23Q8
| PubChem = 25256198
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| ChemSpiderID = 24750794
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<!--Chemical data-->
| C=22 | H=16 | Cl=1 | F=1 | N=6 | O=1
| smiles = C[C@]5(Cc1cncnc1)C(=O)N(c2nc[nH]n2)c4ccc(c3ccc(F)c(Cl)c3)cc45
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'''TROX-1''' is a drug which acts as a potent [[calcium channel blocker|blocker]] of the Ca<sub>v</sub>2 type [[Voltage-dependent calcium channel|calcium channels]]. It was developed as a potential [[analgesic]] after the discovery that the selective [[N-type calcium channel|Ca<sub>v</sub>2.2]] 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|Ca<sub>v</sub>2.1]] and [[R-type calcium channel|Ca<sub>v</sub>2.3]] 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 [[NSAID]]s such as [[naproxen]] or [[diclofenac]], and anti-[[allodynia]] effects equivalent to [[pregabalin]] or [[duloxetine]].<ref name="pmid20439438">{{cite journal | vauthors = 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 | display-authors = 6 | title = Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 334 | issue = 2 | pages = 545–55 | date = August 2010 | pmid = 20439438 | doi = 10.1124/jpet.110.166363 | s2cid = 25588800 }}</ref><ref name="pmid22188924">{{cite journal | vauthors = 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 | display-authors = 6 | title = Characterization of the substituted N-triazole oxindole TROX-1, a small-molecule, state-dependent inhibitor of Ca(V)2 calcium channels | journal = Molecular Pharmacology | volume = 81 | issue = 3 | pages = 488–97 | date = March 2012 | pmid = 22188924 | doi = 10.1124/mol.111.075226 | s2cid = 1617039 }}</ref><ref name="pmid26247695">{{cite journal | vauthors = Rahman W, Patel R, Dickenson AH | title = Electrophysiological evidence for voltage-gated calcium channel 2 (Cav2) modulation of mechano- and thermosensitive spinal neuronal responses in a rat model of osteoarthritis | journal = Neuroscience | volume = 305 | pages = 76–85 | date = October 2015 | pmid = 26247695 | pmc = 4564012 | doi = 10.1016/j.neuroscience.2015.07.073 }}</ref>
== References ==
{{reflist}}
{{Calcium channel blockers}}
[[Category:Calcium channel blockers]]
{{cardiovascular-drug-stub}}