TargetMol

GSK172981

Product Code:
 
TAR-T32004
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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Further Information

Bioactivity:
GSK172981 is a non-peptide tachykinin NK3 receptor antagonist with a high affinity for the recombinant human (PK (I) value 7.7) and native guinea pig (PK (I) value 7.8) tachykinin NK3 receptor. In vitro, the functional evaluation showed that GSK172981 was a competitive antagonist for the cloned human tachykinin NK(3) receptor (PA (2)=7.2). GSK172981 may be used to treat schizophrenia.
CAS:
1133705-99-3
Molecular Weight:
411.47
Purity:
0.98
SMILES:
C(N[C@@H]([C@@H]1CC1)C2=CC=CC=C2)(=O)C=3C4=C(N=C(C3N)C5=CC(F)=CC=C5)C=CC=C4

References

Smith PW, Wyman PA, Lovell P, Goodacre C, Serafinowska HT, Vong A, Harrington F, Flynn S, Bradley DM, Porter R, Coggon S, Murkitt G, Searle K, Thomas DR, Watson JM, Martin W, Wu Z, Dawson LA. New quinoline NK3 receptor antagonists with CNS activity. Bioorg Med Chem Lett. 2009 Feb 1;19(3):837-40. doi: 10.1016/j.bmcl.2008.12.005. Epub 2008 Dec 7. PubMed PMID: 19117759. Dawson LA, Langmead CJ, Dada A, Watson JM, Wu Z, de la Flor R, Jones GA, Cluderay JE, Southam E, Murkitt GS, Hill MD, Jones DN, Davies CH, Hagan JJ, Smith PW. In vitro and in vivo comparison of two non-peptide tachykinin NK3 receptor antagonists: Improvements in efficacy achieved through enhanced brain penetration or altered pharmacological characteristics. Eur J Pharmacol. 2010 Feb 10;627(1-3):106-14. doi: 10.1016/j.ejphar.2009.10.054. Epub 2009 Oct 30. PubMed PMID: 19879867.