Potent and selective nociceptin/orphanin FQ (NOP) receptor antagonist (pA2
= 7.75). Displays selectivity for NOP receptors over classical opioid receptors (pKi
values are 8.65, 6.60, 6.14 and < 5 for NOP, μ
-, and δ
-opioid receptors respectively). Attenuates motor deficits in a rat model of Parkinson's Disease. Active in vivo
Soluble to 50 mM in DMSO
Store at +4°C
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Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist.
Trapella et al.
The novel nociceptin/orphanin FQ receptor antagonist Trap-101 alleviates experimental parkinsonism through inhibition of the nigro-thalamic pathway: positive interaction with L-DOPA.
Marti et al.