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Details

Stereochemistry ABSOLUTE
Molecular Formula C39H49ClN4O2
Molecular Weight 641.285
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GSK-1004723

SMILES

ClC1=CC=C(CC2=NN(C[C@H]3CCCN3CCCCC4=CC=C(OCCCN5CCCCCC5)C=C4)C(=O)C6=C2C=CC=C6)C=C1

InChI

InChIKey=YANGEESWIGIKOP-UUWRZZSWSA-N
InChI=1S/C39H49ClN4O2/c40-33-19-15-32(16-20-33)29-38-36-13-3-4-14-37(36)39(45)44(41-38)30-34-12-9-27-43(34)26-8-5-11-31-17-21-35(22-18-31)46-28-10-25-42-23-6-1-2-7-24-42/h3-4,13-22,34H,1-2,5-12,23-30H2/t34-/m1/s1

HIDE SMILES / InChI

Molecular Formula C39H49ClN4O2
Molecular Weight 641.285
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

GSK-1004723 is a dual histamine H(1) and H(3) receptor antagonist with a long duration of action that has been investigated for the treatment of allergic rhinitis. GSK-1004723 was designed for intranasal administration as a suspension or solution. Clinical trials (phase 1 and 2) showed that GSK-1004723 is well tolerated and demonstrates clinically significant attenuation of symptoms (tested in an environmental allergen challenge chamber). However, attenuation of symptoms was less than seen for treatment with cetirizine (a commonly used over-the-counter antihistamine).

Originator

Approval Year

Patents

Patents

Substance Class Chemical
Created
by admin
on Mon Mar 31 21:16:15 GMT 2025
Edited
by admin
on Mon Mar 31 21:16:15 GMT 2025
Record UNII
S08212J4ZR
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GSK1004723
Preferred Name English
GSK-1004723
Common Name English
1(2H)-PHTHALAZINONE, 4-((4-CHLOROPHENYL)METHYL)-2-(((2R)-1-(4-(4-(3-(HEXAHYDRO-1H-AZEPIN-1-YL)PROPOXY)PHENYL)BUTYL)-2-PYRROLIDINYL)METHYL)-
Systematic Name English
Code System Code Type Description
CAS
955359-72-5
Created by admin on Mon Mar 31 21:16:15 GMT 2025 , Edited by admin on Mon Mar 31 21:16:15 GMT 2025
PRIMARY
DRUG BANK
DB12806
Created by admin on Mon Mar 31 21:16:15 GMT 2025 , Edited by admin on Mon Mar 31 21:16:15 GMT 2025
PRIMARY
PUBCHEM
17747460
Created by admin on Mon Mar 31 21:16:15 GMT 2025 , Edited by admin on Mon Mar 31 21:16:15 GMT 2025
PRIMARY
FDA UNII
S08212J4ZR
Created by admin on Mon Mar 31 21:16:15 GMT 2025 , Edited by admin on Mon Mar 31 21:16:15 GMT 2025
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Long acting slowly dissociates.
Ki
TARGET -> INHIBITOR
Long acting slowly dissociates.
BINDING
Ki
Related Record Type Details
ACTIVE MOIETY