GSK172981
CAS No. : 1133705-99-3
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| Cat. No. : | HY-121164 |
| M.Wt: | 411.47 |
| Formula: | C26H22FN3O |
| Purity: | >98 % |
| Solubility: |
GSK172981 is a brain-penetrant tachykinin NK3 receptor antagonist with pKi 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: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 pKB = 8.1)[1]. In Vivo:Acute GSK172981 (30 mg/kg, i.p.) attenuates Haloperidol (HY-14538)-induced increases in extracellular dopamine in the guinea pig nucleus accumbens[1]
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