GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pKi of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB) (HY-P0242)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia[1][2].
Molekulargewicht:
499.62
CAS Nummer:
[1133706-08-7]
Formel:
C29H29N3O3S
Target-Kategorie:
Neurokinin Receptor
Anwendungsbeschreibung:
MCE Product type: Reference compound
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