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Details

Stereochemistry ACHIRAL
Molecular Formula C12H16ClN3O3S
Molecular Weight 317.792
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DABUZALGRON

SMILES

CC1=C(NS(C)(=O)=O)C(Cl)=CC=C1OCC2=NCCN2

InChI

InChIKey=FOYWMEJSRSBQGB-UHFFFAOYSA-N
InChI=1S/C12H16ClN3O3S/c1-8-10(19-7-11-14-5-6-15-11)4-3-9(13)12(8)16-20(2,17)18/h3-4,16H,5-7H2,1-2H3,(H,14,15)

HIDE SMILES / InChI

Molecular Formula C12H16ClN3O3S
Molecular Weight 317.792
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Dabuzalgron is an orally active and selective alpha1A/1L-adrenoreceptor partial agonist, developed by Roche. In anesthetized micropigs and rabbits, dabuzalgron produced non-selective, dose-dependent increases in intraurethral and arterial blood pressures. In conscious micropigs, both agents produced dose-dependent increases in urethral tension. Dabuzalgron was investigated in a clinical study in women with stress urinary incontinence (SUI). It was demonstrated that 1.5 mg of the drug administered twice daily lead to a significantly lower mean weekly number of SUI episodes with little or no cardiovascular effect. Despite positive results, no development of the drug was reported by Roche.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P35348|||B0ZBD9|||Q6RUJ8
Gene ID: 148.0
Gene Symbol: ADRA1A
Target Organism: Homo sapiens (Human)
21.0 nM [EC50]
PubMed

PubMed

TitleDatePubMed
Pharmacological characteristics of Ro 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist: a potential therapy for stress urinary incontinence.
2004 Jan
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:21:48 GMT 2023
Edited
by admin
on Fri Dec 15 16:21:48 GMT 2023
Record UNII
LGX4GZ74WO
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DABUZALGRON
INN  
INN  
Official Name English
N-(6-CHLORO-3-(4,5-DIHYDRO-1H-IMIDAZOL-2-YLMETHOXY)-2-METHYLPHENYL)METHANESULFONAMIDE
Systematic Name English
METHANESULFONAMIDE, N-(6-CHLORO-3-((4,5-DIHYDRO-1H-IMIDAZOL-2-YL)METHOXY)-2-METHYLPHENYL)-
Systematic Name English
dabuzalgron [INN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29709
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
Code System Code Type Description
CAS
219311-44-1
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
PRIMARY
EPA CompTox
DTXSID50176345
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
PRIMARY
SMS_ID
100000184090
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
PRIMARY
PUBCHEM
216249
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
PRIMARY
INN
8386
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
PRIMARY
CHEBI
142452
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
PRIMARY
MESH
C481520
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
PRIMARY
FDA UNII
LGX4GZ74WO
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
PRIMARY
ChEMBL
CHEMBL257978
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
PRIMARY
NCI_THESAURUS
C75036
Created by admin on Fri Dec 15 16:21:48 GMT 2023 , Edited by admin on Fri Dec 15 16:21:48 GMT 2023
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
TARGET -> AGONIST
Related Record Type Details
ACTIVE MOIETY