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Submit ReviewPotent 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.
M. Wt | 434.02 |
Formula | C24H35N3O2.HCl |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 1216621-00-9 |
PubChem ID | 56972178 |
InChI Key | YEVMLMQAMCKVSC-UHFFFAOYSA-N |
Smiles | Cl.CCN1C(=O)N(C2=CC=CC=C12)C1=C(CO)CN(CC2CCCCCCC2)CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Trapella et al (2006) Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist. Bioorg.Med.Chem. 14 692 PMID: 16202610
Marti et al (2008) 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. 107 1683 PMID: 19014386
Keywords: Trap 101, Trap 101 supplier, Potent, selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioid, Trap101, Parkinsons, disease, antiparkinsons, active, in, vivo, 2508, Tocris Bioscience
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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.