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Chemical Structure : PF-04455242 hydrochloride
Catalog No.: PC-62109Not For Human Use, Lab Use Only.
PF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively.
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PF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively; shows 20-fold reduced affinity for hMOR and negligible affinity for DOR (Ki>4 uM); demonstrates antidepressant-like efficacy, attenuates the behavioral effects of stress, dose-dependently reduceds the elevation of spiradoline-induced plasma prolactin in rats.
Depression
Phase 1 Discontinued
| M.Wt | 408.985 | |
| Formula | C21H29ClN2O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Verhoest PR, et al. J Med Chem. 2011 Aug 25;54(16):5868-77.
2. Grimwood S, et al. J Pharmacol Exp Ther. 2011 Nov;339(2):555-66.
3. Melief EJ, et al. Mol Pharmacol. 2011 Nov;80(5):920-9.
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