TROX-1

From Wikipedia, the free encyclopedia
Jump to: navigation, search
TROX-1
TROX-1 structure.png
Systematic (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
Clinical data
Legal status
?
Identifiers
ATC code ?
PubChem CID 25256198
ChemSpider 24750794
Chemical data
Formula C22H16ClFN6O 
Mol. mass 434.853 g/mol

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 but comparatively milder side effects. 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]

References[edit]

  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 (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.