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TRPV1 antagonist 11

TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC50 of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice[1].

Product Specifications

CAS Number

3084843-71-7

UNSPSC

12352005

Target

Opioid Receptor; TRP Channel

Related Pathways

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

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Smiles

COC1=CC2=C(C(CCNC(N3CCN(CC3)C4=NC=CC(N5CCC(CC5)C6=CC=CC=C6)=N4)=O)=CN2)C=C1

Molecular Formula

C31H37N7O2

Molecular Weight

539.67

References & Citations

[1]Yusui Wang, et al. Design, synthesis and biological activity of novel pyrimidine piperazine ureas as μ-opioid and TRPV1 dual-target ligands for pain management. Eur J Med Chem. 2025 Aug 5:292:117656.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

TRPV1; μ Opioid Receptor/MOR

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