Chemical Name: 1-[1-(Cyclooctylmethyl)-1,2,3,6-tetrahydro-5-(hydroxymethyl)-4-pyridinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one hydrochloride
Biological ActivityPotent 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-, κ-, and δ-opioid receptors respectively). Attenuates motor deficits in a rat model of Parkinson's Disease. Active in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist.
Trapella et al.
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