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GR 159897

Names

[ CAS No. ]:
158848-32-9

[ Name ]:
GR 159897

[Synonym ]:
Tocris-1274
Agitoxin 2
HMS3267L05

Biological Activity

[Description]:

GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide antagonist at tachykinin NK2 receptors, inhibits binding of [3H]GR100679 to hNK2-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction, with anxiolytic-like activity[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor

[Target]

NK2:10 (pKi, Rat colon membrane)

hNK2:9.51 (pKi, CHO cell)


[References]

[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.

Chemical & Physical Properties

[ Density]:
1.29g/cm3

[ Boiling Point ]:
600.2ºC at 760mmHg

[ Molecular Formula ]:
C23H27FN2O2S

[ Molecular Weight ]:
414.54

[ Flash Point ]:
316.8ºC

[ Exact Mass ]:
414.17800

[ PSA ]:
64.54000

[ LogP ]:
4.94190

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.656

Safety Information

[ WGK Germany ]:
3

Related Compounds