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Details

Stereochemistry ACHIRAL
Molecular Formula C12H16ClN3O3S.ClH
Molecular Weight 354.253
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DABUZALGRON HYDROCHLORIDE

SMILES

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

InChI

InChIKey=QFRMKDCRDUXTBR-UHFFFAOYSA-N
InChI=1S/C12H16ClN3O3S.ClH/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);1H

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

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

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
A randomized crossover study to evaluate RO 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist in women with stress urinary incontinence.
2004 Jun
A randomized crossover study to evaluate Ro 115-1240, a selective alpha-adrenoceptor partial agonist in women with stress urinary incontinence.
2004 May
Pharmacological properties of 2-((R-5-chloro-4-methoxymethylindan-1-yl)-1H-imidazole (PF-3774076), a novel and selective alpha1A-adrenergic partial agonist, in in vitro and in vivo models of urethral function.
2009 Sep
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:36:25 GMT 2023
Edited
by admin
on Fri Dec 15 16:36:25 GMT 2023
Record UNII
A7Q00A39MF
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DABUZALGRON HYDROCHLORIDE
USAN  
USAN  
Official Name English
RO-115-1240
Code English
RO115-1240/190
Code English
METHANESULFONAMIDE, N-(6-CHLORO-3-((4,5-DIHYDRO-1H-IMIDAZOL-2-YL)METHOXY)-2-METHYLPHENYL)-, MONOHYDROCHLORIDE
Common Name English
N-(6-CHLORO-3-(4,5-DIHYDRO-1-H-IMIDAZOL-2-YLMETHOXY)-2-METHYLPHENYL)METHANESULFONAMIDE HYDROCHLORIDE
Common Name English
DABUZALGRON HCL
Common Name English
DABUZALGRON HYDROCHLORIDE [USAN]
Common Name English
RS-151240-190
Code English
RO-1151240190
Code English
Classification Tree Code System Code
NCI_THESAURUS C29709
Created by admin on Fri Dec 15 16:36:25 GMT 2023 , Edited by admin on Fri Dec 15 16:36:25 GMT 2023
Code System Code Type Description
SMS_ID
100000184101
Created by admin on Fri Dec 15 16:36:25 GMT 2023 , Edited by admin on Fri Dec 15 16:36:25 GMT 2023
PRIMARY
FDA UNII
A7Q00A39MF
Created by admin on Fri Dec 15 16:36:25 GMT 2023 , Edited by admin on Fri Dec 15 16:36:25 GMT 2023
PRIMARY
ChEMBL
CHEMBL257978
Created by admin on Fri Dec 15 16:36:25 GMT 2023 , Edited by admin on Fri Dec 15 16:36:25 GMT 2023
PRIMARY
PUBCHEM
219093
Created by admin on Fri Dec 15 16:36:25 GMT 2023 , Edited by admin on Fri Dec 15 16:36:25 GMT 2023
PRIMARY
CAS
219311-43-0
Created by admin on Fri Dec 15 16:36:25 GMT 2023 , Edited by admin on Fri Dec 15 16:36:25 GMT 2023
PRIMARY
EPA CompTox
DTXSID90176344
Created by admin on Fri Dec 15 16:36:25 GMT 2023 , Edited by admin on Fri Dec 15 16:36:25 GMT 2023
PRIMARY
USAN
PP-84
Created by admin on Fri Dec 15 16:36:25 GMT 2023 , Edited by admin on Fri Dec 15 16:36:25 GMT 2023
PRIMARY
NCI_THESAURUS
C75037
Created by admin on Fri Dec 15 16:36:25 GMT 2023 , Edited by admin on Fri Dec 15 16:36:25 GMT 2023
PRIMARY
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