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
^Abbadie C, McManus OB, Sun SY, Bugianesi RM, Dai G, Haedo RJ, et al. (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.
PMID20439438.
S2CID25588800.
^Swensen AM, Herrington J, Bugianesi RM, Dai G, Haedo RJ, Ratliff KS, et al. (March 2012). "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.
doi:
10.1124/mol.111.075226.
PMID22188924.
S2CID1617039.