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Details

Stereochemistry ACHIRAL
Molecular Formula C18H20FN3O3S
Molecular Weight 377.433
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of R-1485

SMILES

FC1=C(C=CC=C1)S(=O)(=O)N2CCOC3=C2C=CC=C3N4CCNCC4

InChI

InChIKey=UPROBLPRPWYJGN-UHFFFAOYSA-N
InChI=1S/C18H20FN3O3S/c19-14-4-1-2-7-17(14)26(23,24)22-12-13-25-18-15(5-3-6-16(18)22)21-10-8-20-9-11-21/h1-7,20H,8-13H2

HIDE SMILES / InChI

Description
Curator's Comment: Description was created based on several sources, including https://www.tocris.com/dispprod.php?ItemId=385007#.WH5ExlOLSwU

R-1485 is a lead candidate identified from Roche Pharmaceuticals research programme for the treatment of Alzheimer's disease. Selective and high affinity 5-HT6 antagonist; displays low hERG inhibition. Exhibits >100 fold selectivity against a panel of 50 targets including other 5-HT receptor subtypes. R-1485 is currently in Phase I trials at Roche for the treatment of Alzheimer’s type dementia. This compound showed a pKi value of 9.3 when it was tested for inhibition of [3H]-LSD binding to human 5-HT6 receptors expressed in HEK293 cells. In addition, it was also found that in rats this agent has good BBB permeability.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
5-hydroxytryptamine subtype 6 receptor modulators: a patent survey.
2010 Sep
Patents

Patents

Sample Use Guides

In Vivo Use Guide
Unknown
Route of Administration: Unknown
In Vitro Use Guide
Unknown
Name Type Language
R-1485
Code English
4-((2-FLUOROPHENYL)SULFONYL)-3,4-DIHYDRO-8-(1-PIPERAZINYL)-2H-1,4-BENZOXAZINE
Systematic Name English
R 1485
Code English
4-(2-FLUOROPHENYL)SULFONYL-8-PIPERAZIN-1-YL-2,3-DIHYDRO-1,4-BENZOXAZINE
Systematic Name English
2H-1,4-BENZOXAZINE, 4-((2-FLUOROPHENYL)SULFONYL)-3,4-DIHYDRO-8-(1-PIPERAZINYL)-
Systematic Name English
Code System Code Type Description
CAS
788155-53-3
Created by admin on Sat Dec 16 09:42:00 GMT 2023 , Edited by admin on Sat Dec 16 09:42:00 GMT 2023
PRIMARY
PUBCHEM
11689373
Created by admin on Sat Dec 16 09:42:00 GMT 2023 , Edited by admin on Sat Dec 16 09:42:00 GMT 2023
PRIMARY
FDA UNII
B254UB9ZBA
Created by admin on Sat Dec 16 09:42:00 GMT 2023 , Edited by admin on Sat Dec 16 09:42:00 GMT 2023
PRIMARY