DABUZALGRON HYDROCHLORIDE

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 Search

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/14678390 | https://www.ncbi.nlm.nih.gov/pubmed/14678373

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

Primary Target	Pharmacology	Condition	Potency
Alpha-1A adrenergic receptor 19 Target ID: P35348\|\|\|B0ZBD9\|\|\|Q6RUJ8 Gene ID: 148.0 Gene Symbol: ADRA1A Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/28286875	Agonist 2678		21.0 nM [EC50]

PubMed

Title	Date	PubMed
Pharmacological characteristics of Ro 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist: a potential therapy for stress urinary incontinence.	2004 Jan	14678390
A randomized crossover study to evaluate Ro 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist in women with stress urinary incontinence.	2004 Jan	14678373
A randomized crossover study to evaluate RO 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist in women with stress urinary incontinence.	2004 Jun	15180647
A randomized crossover study to evaluate Ro 115-1240, a selective alpha-adrenoceptor partial agonist in women with stress urinary incontinence.	2004 May	15142177
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	19498105

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

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Name

Type

Language

DABUZALGRON HYDROCHLORIDE

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