XEN-2174

XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating α2-adrenergic receptor at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research[1].

Product Specifications

CAS Number

[701909-57-1]

UNSPSC

12352005

Target

Adrenergic Receptor; Monoamine Transporter

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling

Field of Research

Neurological Disease

Smiles

O=C1N2[C@](C[C@H](C2)O)([H])C(N[C@@H](CSSC[C@@H](C(N[C@@]3([H])CSSC[C@@](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC3=O)=O)CC4=CC=C(C=C4)O)=O)CCCCN)=O)CC(C)C)=O)([H])C(N[C@H]1CC5=CN=CN5)=O)=O)NC([C@H](C(C)C)NC(CNC([C@@H]6CCC(N6)=O)=O)=O)=O)C(N)=O)=O

Molecular Formula

C58H85N17O16S4

Molecular Weight

1404.66

References & Citations

[1]Okkerse P, et al. Pharmacokinetics and pharmacodynamics of intrathecally administered Xen2174, a synthetic conopeptide with norepinephrine reuptake inhibitor and analgesic properties. Br J Clin Pharmacol. 2017 Apr;83 (4) :751-763.