158848-32-9
Chemical Structure
GR 159897
- CAS No.: 158848-32-9
- Formula:C23H27FN2O2S
- Molecular Weight:414.54
IUPAC Name: (R)-5-fluoro-3-(2-(4-methoxy-4-((phenylsulfinyl)methyl)piperidin-1-yl)ethyl)-1H-indole
InChIKey: BANYJBHWTOJQDU-GDLZYMKVSA-N
SMILES: O=[S@](CC1(OC)CCN(CCC2=CNC3=C2C=C(F)C=C3)CC1)C4=CC=CC=C4
Biological Activity: 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].
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GR 159897 | 99.6% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
