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Details

Stereochemistry ACHIRAL
Molecular Formula C12H12Cl2N2O.ClH
Molecular Weight 307.603
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PBT-1033 HYDROCHLORIDE

SMILES

Cl.CN(C)CC1=NC2=C(O)C(Cl)=CC(Cl)=C2C=C1

InChI

InChIKey=VSRSUNAZJQGYCB-UHFFFAOYSA-N
InChI=1S/C12H12Cl2N2O.ClH/c1-16(2)6-7-3-4-8-9(13)5-10(14)12(17)11(8)15-7;/h3-5,17H,6H2,1-2H3;1H

HIDE SMILES / InChI

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C12H12Cl2N2O
Molecular Weight 271.142
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

PBT-1033, also known as PBT-2, is a neural protective agent potentially for the treatment of Alzheimer's disease and Huntington's Disease. PBT-1033 is a moderate-affinity 8-hydroxyquinoline transition metal-ligand that acts as a synthetic chaperone, re distributing copper, zinc, and iron from locations where they are abundant to subcellular locations where they might be deficient. Delivery of copper and zinc by PBT-1033 into the cytoplasm deactivates the kinase glycogen synthase kinase 3β and the phosphatase calcineurin, both potential targets for Huntington’s disease. In aged wild-type mice, PBT-1033 improves cognitive ability and markers of neuronal plasticity and function. In Alzheimer’s disease mouse models, PBT-1033 inhibits the accumulation of amyloid β, attenuates neuropathological effects of amyloid β, including amyloid-β-induced hyperphosphorylation of tau, and improves cognition. In a 12-week, phase 2a, randomized, double-blind, placebo-controlled trial in 78 individuals with mild Alzheimer’s dementia, PBT-1033 was safe and well tolerated and significantly reduced concentrations of amyloid β42 in CSF.

Approval Year

PubMed

PubMed

TitleDatePubMed

Sample Use Guides

once daily 250 mg
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Sat Dec 16 12:56:56 UTC 2023
Edited
by admin
on Sat Dec 16 12:56:56 UTC 2023
Record UNII
24Z79C941B
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PBT-1033 HYDROCHLORIDE
Common Name English
PBT2 HYDROCHLORIDE
Code English
8-QUINOLINOL, 5,7-DICHLORO-2-((DIMETHYLAMINO)METHYL)-, HYDROCHLORIDE (1:1)
Systematic Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 353711
Created by admin on Sat Dec 16 12:56:56 UTC 2023 , Edited by admin on Sat Dec 16 12:56:56 UTC 2023
EU-Orphan Drug EU/3/15/1497
Created by admin on Sat Dec 16 12:56:56 UTC 2023 , Edited by admin on Sat Dec 16 12:56:56 UTC 2023
Code System Code Type Description
PUBCHEM
46911781
Created by admin on Sat Dec 16 12:56:56 UTC 2023 , Edited by admin on Sat Dec 16 12:56:56 UTC 2023
PRIMARY
EVMPD
SUB196790
Created by admin on Sat Dec 16 12:56:56 UTC 2023 , Edited by admin on Sat Dec 16 12:56:56 UTC 2023
PRIMARY
SMS_ID
100000182616
Created by admin on Sat Dec 16 12:56:56 UTC 2023 , Edited by admin on Sat Dec 16 12:56:56 UTC 2023
PRIMARY
CAS
648896-70-2
Created by admin on Sat Dec 16 12:56:56 UTC 2023 , Edited by admin on Sat Dec 16 12:56:56 UTC 2023
PRIMARY
FDA UNII
24Z79C941B
Created by admin on Sat Dec 16 12:56:56 UTC 2023 , Edited by admin on Sat Dec 16 12:56:56 UTC 2023
PRIMARY
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ACTIVE MOIETY