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7-DICHLORO-2-DIMETHYLAMINOMETHYL-QUINOLIN-8-OL

Names

[ CAS No. ]:
747408-78-2

[ Name ]:
7-DICHLORO-2-DIMETHYLAMINOMETHYL-QUINOLIN-8-OL

[Synonym ]:
5,7-Dichloro-2-[(dimethylamino)methyl]-8-quinolinol
Q7K6GJQ4O4
8-Quinolinol, 5,7-dichloro-2-[(dimethylamino)methyl]-
PBT-1033
MFCD30749371

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[In Vitro]

PB 1033 displays antibacterial activity against S. uberis, with a MIC value of 14.5 μM[2]. PBT2 (1, 3 and 7.5 μM, 6 h) protects neurons against glutamate-induced excitotoxicity[3]. PBT2 (10 μM, 1 or 6 h) reduces NMDAR-mediated Ca2+ flux in mouse cortical neurons[3]. PBT2 (0-10 μM, 1 h) increases GSK3α/β phosphorylation in SH-SY5Y cells[4]. PBT2 (20 μM, 1 h) prevents the formation of Zn-induced protease resistant Aβ aggregates[5]. Western Blot Analysis[4] Cell Line: SH-SY5Y cells Concentration: 0-10 μM Incubation Time: 1 h Result: Increased in cellular levels of GSK3α/β phosphorylated at the inhibitory serine 21/9 residue (ser21/9 on GSK3α/β).

[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.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
367.8±37.0 °C at 760 mmHg

[ Molecular Formula ]:
C12H12Cl2N2O

[ Molecular Weight ]:
271.142

[ Flash Point ]:
176.2±26.5 °C

[ Exact Mass ]:
270.032654

[ LogP ]:
3.51

[ Vapour Pressure ]:
0.0±0.9 mmHg at 25°C

[ Index of Refraction ]:
1.654


Related Compounds