GSK172981 

GSK172981 is a brain-penetrant tachykinin NK3 receptor antagonist with pK_i values of 7.7 and 7.8 for human and native guinea pig NK3 receptors, respectively. GSK172981 can be used for the study of schizophrenia^[1].

In vitro functional evaluations revealed GSK172981 to be a competitive antagonist (pA₂ = 7.2) at cloned human tachykinin NK3 receptor. GSK172981 also exhibits a competitive profile in antagonizing neurokinin B-stimulated neuronal activity recorded from the guinea pig medial habenula slices (apparent pK_B = 8.1)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Acute GSK172981 (30 mg/kg, i.p.) attenuates Haloperidol (HY-14538)-induced increases in extracellular dopamine in the guinea pig nucleus accumbens^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

411.47

C₂₆H₂₂FN₃O

1133705-99-3

O=C(N[C@H](C1=CC=CC=C1)C2CC2)C3=C(C(C4=CC=CC(F)=C4)=NC5=CC=CC=C35)N

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Dawson LA, et al. 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.  [Content Brief]