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GSK256471

CAT: 0804-HY-116268Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-116268Size:1 Each
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Description
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) -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].
CAS Number
1133706-08-7
UNSPSC
12352005
Target
Neurokinin Receptor
Related Pathways
GPCR/G Protein; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Smiles
O=C(N[C@H](C1=CC=CC=C1)C2CC2)C3=C(C(C4=CC=CC=C4)=NC5=CC=CC=C35)CN(S(=O)(C)=O)C
Molecular Formula
C29H29N3O3S
Molecular Weight
499.62
References & Citations
[1]Smith PW, et al. New quinoline NK3 receptor antagonists with CNS activity. Bioorg Med Chem Lett. 2009 Feb 1;19 (3) :837-40. |[2]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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
NK3R

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