A nonpeptide NK2 receptor antagonist
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GR159897

Item No. 32774

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-1H-indole
CAS Number
158848-32-9
Molecular Formula
C23H27FN2O2S
Formula Weight
414.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/ml
SMILES
O=[S@@](C1=CC=CC=C1)CC(OC)(CC2)CCN2CCC(C3=C4)=CNC3=CC=C4F
InChi Code
InChI=1S/C23H27FN2O2S/c1-28-23(17-29(27)20-5-3-2-4-6-20)10-13-26(14-11-23)12-9-18-16-25-22-8-7-19(24)15-21(18)22/h2-8,15-16,25H,9-14,17H2,1H3/t29-/m1/s1
InChi Key
BANYJBHWTOJQDU-GDLZYMKVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $202

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    10 mg

    $283

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    Product Description

    GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK2) receptor.1 It binds to NK2 receptors (Ki = 0.32 nM) and is selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK2 receptor agonist GR64349 in isolated guinea pig trachea (pA2 = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Beresford, I.J., Sheldrick, R.L., Ball, D.I., et al. GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur. J. Pharmacol. 272(2-3), 241-248 (1995).

    2. Walsh, D.M., Stratton, S.C., Harvey, F.J., et al. The anxiolytic-like activity of GR159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety. Psychopharmacol. (Berl) 121(2), 186-191 (1995).