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GR-159897

Chemical Structure : GR-159897

CAS No.: 158848-32-9

GR-159897 (GR159897;GR-159897)

Catalog No.: PC-70192Not For Human Use, Lab Use Only.

A potent non-peptide antagonist of tachykinin NK2 receptor with pKi of 9.5 in CHO cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent non-peptide antagonist of tachykinin NK2 receptor with pKi of 9.5 in CHO cells; competitively antagonises the contractions induced by GR64349 in guinea-pig trachea (pA2 8.7); has negligible activity at human NK1 (pKi<5); potently antagonises bronchoconstriction induced by GR6434 in the anaesthetised guinea-pig; shows anxiolytic effects in animal models.

Physicochemical Properties

M.Wt 414.535
Formula C23H27FN2O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-1H-indole

References

1. Beresford IJ, et al. Eur J Pharmacol. 1995 Jan 16;272(2-3):241-8.

2. Walsh DM, et al. Psychopharmacology (Berl). 1995 Sep;121(2):186-91.

3. Advenier C. Can J Physiol Pharmacol. 1995 Jul;73(7):878-84.

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