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GR 159897
- Optical Purity: 98% e.e.
- Soluble in DMSO
- MF: C23H27FN2O2S
- MW: 414.54
Description
GR 159897 is a potent and selective non-peptide neurokinin NK2 receptor antagonist with high affinity pKi values near 9.5. It is suitable for blocking tachykinin NK2 receptor-mediated responses in functional assays. It crosses the blood-brain barrier and exhibits strong anti-tumor, anti-stress, and anxiolytic (anti-anxiety) properties.
NK2 receptors are activated primarily by neurokinin A and participate in smooth muscle contraction, airway responses and visceral signaling. GR 159897 is a useful antagonist for tachykinin receptor pharmacology and inflammation-related pathway studies.
Key Features
- Potent non-peptide NK2 receptor antagonist
- Selective on NK2 with pKi values near 9.5, with little to no affinity for NK1 or NK3 receptors
- Blocks tachykinin-mediated NK2 signaling
- Useful for smooth muscle and visceral response studies
Applications
- NK2 receptor pharmacology
- Tachykinin signaling research
- Airway and smooth muscle contraction models
- Visceral pain and inflammation pathway studies
More Information
| Parent CAS No. | 158848-32-9 |
|---|---|
| Chemical Name | 3-[2-(4-(R)-Benzenesulfinylmethyl-4-methoxy-piperidin-1-yl)-ethyl]-5-fluoro-1H-indole |
| SMILES | C1NC2C=CC(F)=CC=2C=1CCN1CCC(OC)(C[S@+](C2C=CC=CC=2)[O-])CC1 |&1:19,r| |
| MFCD | N.A. |
| InChi | 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 |
| InChiKey | BANYJBHWTOJQDU-GDLZYMKVSA-N |
| CID | 9953599 |
| Short Description | NK2 antagonist |
References
- DM Walsh et al. The anxiolytic-like activity of GR 159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety. Psychopharmacol. 1995, 121, 186-191.
- AWJ Cooper et al. GR 159897 and related analogues as highly potent, orally active non-peptide neurokinin NK2 receptor antagonists. Bioorg. Med. Chem. Lett. 1994, 4(16), 1951.
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