2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. 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.

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R116031

R116031 Chemical Structure

CAS No. : 336884-84-5

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Description

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].

Molecular Weight

660.69

Formula

C35H38F6N4O2
CAS No.
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
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R116031 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

R116031336884-84-5R 116031R-116031Neurokinin ReceptorNK receptorTachykinin receptorNK-1 receptorPeripheral effectsCentral effectPET ligandInhibitorinhibitorinhibit

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