Identification | Back Directory | [Name]
2(1H)-Pyridinone, 1-(4-fluorophenyl)-4-[(2S)-2-phenoxypropoxy]- | [CAS]
2126784-39-0 | [Synonyms]
2(1H)-Pyridinone, 1-(4-fluorophenyl)-4-[(2S)-2-phenoxypropoxy]- | [Molecular Formula]
C20H18FNO3 | [MOL File]
2126784-39-0.mol | [Molecular Weight]
339.36 |
Chemical Properties | Back Directory | [Boiling point ]
519.9±50.0 °C(Predicted) | [density ]
1.25±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
-1.25±0.63(Predicted) | [color ]
Off-white to light yellow |
Hazard Information | Back Directory | [Description]
VU 6010572 is a negative allosteric modulator (NAM) for mGlu. VU 6010572 has an IC50 of 245 nM for mGlu3 with high selectivity among all mGlu receptors. VU 6010572 is highly CNS penetrant. | [Uses]
VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant[1][2]. | [in vivo]
VU6010572 (3 mg/kg; i.p.) shows robust efficacy[1].
VU6010572 (3 mg/kg; i.p.; 45 minutes) produces lasting anxiolytic-like behavioral effects[2]. Animal Model: | CD-1 mice[1] | Dosage: | 3 mg/kg | Administration: | I.p. | Result: | Showed robust efficacy.
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Animal Model: | Rats[2] | Dosage: | 3 mg/kg | Administration: | I.p.; 45 minutes | Result: | Produced lasting anxiolytic-like behavioral effects.
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| [IC 50]
mGluR3: 245 nM (IC50) | [References]
[1] Engers JL, et al. Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs. ACS Med Chem Lett. 2017;8(9):925-930. Published 2017 Aug 15. DOI:10.1021/acsmedchemlett.7b00249 [2] Ryan E. Tyler1, et al. The effects of predator odor (TMT) exposure and mGlu3 NAM pretreatment on lasting behavioral and molecular adaptations in the insular cortex and BNST |
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