Trap 101

Names

[ Name ]:
Trap 101

[Synonym ]:
1-[1-(Cyclooctylmethyl)-5-(hydroxymethyl)-1,2,3,6-tetrahydro-4-py ridinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one hydrochloride (1:1)

Biological Activity

[Description]:

Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor

Signaling Pathways >> Neuronal Signaling >> Opioid Receptor

Research Areas >> Neurological Disease

[Target]

pKi: 8.65 (NOP receptor); 6.60 (μ-opioid receptor); 6.14 (κ-opioid receptor); < 5 (δ-opioid receptor)[1]

[In Vitro]

Trap-101 hydrochloride (3, 30, and 300 nM) is inactive per se up to 10 μM, while in the range 3-300 nM, it produces a concentration dependent rightward shift of the concentration-response curve to N/OFQ without modifications of the maximal response to the agonist. Receptor binding affinities of Trap101 (pKi values) at recombinant human NOP, and classical opioid receptors expressed in CHO cell membranes are 8.65, 6.60, 6.14 and < 5 for NOP, μ-, κ-, and δ-opioid receptors respectively[1].

[In Vivo]

Trap-101 hydrochloride (10-30 mg/kg; detected after 90 min) changes motor activity in naïve rats, it causes a delayed increase in the immobility time in the bar test at 30 mg/kg, Moreover, it increased stepping activity and rotarod performance at 10 mg/kg and reduces them at 30 mg/kg[1]. 6-OHDA lesioning produces motor asymmetry mostly affecting the contralateral paw and overall reduced motor performance. Trap-101 hydrochloride (intraperitoneal injection; 10-30 mg/kg; detected after 90 min) alleviates akinesia/bradykinesia and improves overall gait ability in hemiparkinsonian rats, being effective starting at 1 mg/kg and without worsening motor deficit at 30 mg/kg[1]. Animal Model: 6-OHDA hemilesioned rats[1] Dosage: 10-30 mg/kg Administration: Intraperitoneal injection; 10-30 mg/kg; detected after 90 min Result: Attenuated parkinsonian-like motor deficits in rat.

[References]

[1]. Matteo Marti, 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. J Neurochem. 2008 Dec;107(6):1683-96.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₃₆ClN₃O₂

[ Molecular Weight ]:
434.01500

[ Exact Mass ]:
433.25000

[ PSA ]:
50.40000

[ LogP ]:
4.83240

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII

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