1001389-72-5
Chemical Structure
GSK-1482160
- CAS No.: 1001389-72-5
- Formula:C14H14ClF3N2O2
- Molecular Weight:334.72
IUPAC Name: (S)-N-(2-chloro-3-(trifluoromethyl)benzyl)-1-methyl-5-oxopyrrolidine-2-carboxamide
InChIKey: BJEMSIVBBUBXMZ-JTQLQIEISA-N
SMILES: O=C([C@H](CC1)N(C)C1=O)NCC2=CC=CC(C(F)(F)F)=C2Cl
Biological Activity: GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI)[1][2][3].
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GSK-1482160 | 98.67% | GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI). | ||||||||||||||||||||
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- [1]. Ali Z, et al. Pharmacokinetic and pharmacodynamic profiling of a P2X7 receptor allosteric modulator GSK1482160 in healthy human subjects. Br J Clin Pharmacol. 2013;75(1):197-207. doi:10.1111/j.1365-2125.2012.04320.x
- [2]. Abdi MH, et al. Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5080-4. [Content Brief]
- [3]. Liu X, et al. Unlocking the therapeutic potential of P2X7 receptor: a comprehensive review of its role in neurodegenerative disorders. Front Pharmacol. 2024 Jul 30;15:1450704. [Content Brief]
Keywords
