GR 159897

GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2) -CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects[1][2].

Product Specifications

CAS Number

[158848-32-9]

UNSPSC

12352005

Target

Neurokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cancer; Endocrinology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gr-159897.html

Purity

99.60

Solubility

DMSO : 31 mg/mL (ultrasonic; warming)

Smiles

O=[S@](CC1(OC)CCN(CCC2=CNC3=C2C=C(F)C=C3)CC1)C4=CC=CC=C4

Molecular Formula

C23H27FN2O2S

Molecular Weight

414.54

References & Citations

[1]Beresford IJ, et al. GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur J Pharmacol. 1995 Jan 16;272 (2-3) :241-8.|[2]Nizam E, et al. Differential consequences of neurokinin receptor 1 and 2 antagonists in metastatic breast carcinoma cells; Effects independent of Substance P. Biomed Pharmacother. 2018 Dec;108:263-270.