TROX-1

TROX-1

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
Identifiers
PubChem	CID: 25256198
ChemSpider	24750794
Chemical data
Formula	C22H16ClFN6O
Molecular mass	434.853 g/mol
SMILES c5ncncc5CC(C)(C2=O)c1cc(-c(cc3Cl)ccc3F)ccc1N2c4nncn4

TROX-1 is a drug which acts as a potent blocker of the Ca_v2 type calcium channels. It was developed as a potential analgesic after the discovery that the selective Ca_v2.2 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 Ca_v2.1 and Ca_v2.3 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.