R116031

R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist with a Ki of 0.45 nM for human NK-1 receptor. R116031 inhibits Substance P (HY-P0201) -induced peripheral effects (skin reactions and plasma extravasation in guinea pigs) and a central effect (thumping in gerbils) .R116031 labeled with 3H significantly accumulate in the striatum, olfactory tubercule, olfactory bulb and locus coeruleus in gerbils models. R116031 can be used as a positron emission tomography (PET) ligand for PET imaging[1].

Product Specifications

CAS Number

[336884-84-5]

UNSPSC

12352005

Target

Neurokinin Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Neurological Disease

Smiles

O=C(C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)N2[C@@H](C[C@@H](N3CCN(CC3)CC(NC4=C(C=CC=C4C)C)=O)CC2)CC5=CC=CC=C5

Molecular Formula

C35H38F6N4O2

Molecular Weight

660.69

References & Citations

[1]Van der Mey M, et al. Synthesis and biodistribution of [ (11) C]R116301, a promising PET ligand for central NK (1) receptors. Bioorg Med Chem. 2005 Mar 1;13 (5) :1579-86.