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

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5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole Basic information
Product Name:5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole
Synonyms:5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-1H-indole;5-Fluoro-3-[2-[4-methoxy-4-[[-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole;GR 159897;(R)-5-Fluoro-3-[2-[4-methoxy-4-[(phenylsulfinyl)methyl]-1-piperidinyl]ethyl]-1H-indole;1H-Indole, 5-fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-;5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole
CAS:158848-32-9
MF:C23H27FN2O2S
MW:414.54
EINECS:
Product Categories:
Mol File:158848-32-9.mol
5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole Structure
5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole Chemical Properties
Boiling point 600.2±55.0 °C(Predicted)
density 1.29±0.1 g/cm3(Predicted)
storage temp. −20°C
solubility DMSO: ~24 mg/mL, soluble
pka16.46±0.30(Predicted)
form solid
color off-white
Safety Information
WGK Germany 3
MSDS Information
ProviderLanguage
SigmaAldrich English
5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole Usage And Synthesis
UsesGR 159897 is an NK2 receptor antagonist which aids in the treatment of IBS.
Biological ActivityA potent, selective, non-peptide, orally active neurokinin NK 2 receptor antagonist. Competes for binding of [ 3 H]GR100679 to hNK 2 -transfected CHO cells with a pK i of 9.5. Inhibits NK 2 receptor-mediated contraction of guinea pig trachea with a pA 2 of 8.7. Anxiolytic in vivo .
in vivo

GR 159897 (0.12 mg/kg; intravenous injection; guinea-pigs) treatment potently antagonizes bronchoconstriction induced by GR64349, with a long duration of action (3 h)[1].

Animal Model:Guinea-pigs[1]
Dosage:0.12 mg/kg
Administration:Intravenous injection
Result:Potently antagonised bronchoconstriction induced by GR64349, with a long duration of action (3 h).
IC 50NK2: 10 (pKi, Rat colon membrane); hNK2: 9.51 (pKi, CHO cell)
storageDesiccate at -20°C
5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole Preparation Products And Raw materials
Tag:5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole(158848-32-9) Related Product Information
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