| Identification | Back Directory | [Name]
7-DICHLORO-2-DIMETHYLAMINOMETHYL-QUINOLIN-8-OL | [CAS]
747408-78-2 | [Synonyms]
PB 1033
7-DICHLORO-2-DIMETHYLAMINOMETHYL-QUINOLIN-8-OL
8-Quinolinol,5,7-dichloro-2-[(dimethylamino)methyl]- | [Molecular Formula]
C12H12Cl2N2O | [MDL Number]
MFCD30749371 | [MOL File]
747408-78-2.mol | [Molecular Weight]
271.14 |
| Chemical Properties | Back Directory | [Boiling point ]
367.8±37.0 °C(Predicted) | [density ]
1.385±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (368.81 mM; Need ultrasonic) | [form ]
Solid | [pka]
7.26±0.28(Predicted) | [color ]
Light yellow to brown |
| Hazard Information | Back Directory | [Uses]
PBT 1033 (PBT 2) is an orally active copper/zinc ionophore. PBT 1033 restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria[1][2]. | [in vivo]
PBT 1033 (30 mg/kg/d, p.o., 11 days) restores biochemical substrates of learning/memory in a mouse model of alzheimer's disease[5].
| Animal Model: | Female Tg2576 mice[5] | | Dosage: | 30 mg/kg/d | | Administration: | Oral administration, 11 days | | Result: | Increased hippocampal apical spine density, basal spine density.
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| [References]
[1] Faux NG, et al. PBT2 rapidly improves cognition in Alzheimer's Disease: additional phase II analyses. J Alzheimers Dis. 2010;20(2):509-16. DOI:10.3233/JAD-2010-1390
[2] Harbison-Price N, et al. Multiple Bactericidal Mechanisms of the Zinc Ionophore PBT2. mSphere. 2020 Mar 18;5(2):e00157-20.
[3] Johanssen T, et al. PBT2 inhibits glutamate-induced excitotoxicity in neurons through metal-mediated preconditioning. Neurobiol Dis. 2015 Sep;81:176-85. DOI:10.1016/j.nbd.2015.02.008
[4] Crouch PJ, et al. The Alzheimer's therapeutic PBT2 promotes amyloid-β degradation and GSK3 phosphorylation via a metal chaperone activity. J Neurochem. 2011 Oct;119(1):220-30. DOI:10.1111/j.1471-4159.2011.07402.x
[5] Adlard PA, et al. Metal ionophore treatment restores dendritic spine density and synaptic protein levels in a mouse model of Alzheimer's disease. PLoS One. 2011 Mar 11;6(3):e17669. DOI:10.1371/journal.pone.0017669 |
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