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
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)
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
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
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 |
21.0 nM [EC50] |
PubMed
Title | Date | PubMed |
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Pharmacological characteristics of Ro 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist: a potential therapy for stress urinary incontinence. | 2004 Jan |
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A randomized crossover study to evaluate RO 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist in women with stress urinary incontinence. | 2004 Jun |
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A randomized crossover study to evaluate Ro 115-1240, a selective alpha-adrenoceptor partial agonist in women with stress urinary incontinence. | 2004 May |
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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
Edited
Wed Jul 05 23:48:19 UTC 2023
by
admin
on
Wed Jul 05 23:48:19 UTC 2023
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Record UNII |
LGX4GZ74WO
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Record Status |
Validated (UNII)
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Record Version |
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Official Name | English | ||
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Systematic Name | English | ||
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NCI_THESAURUS |
C29709
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219311-44-1
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DTXSID50176345
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100000184090
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216249
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8386
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142452
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C481520
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LGX4GZ74WO
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CHEMBL257978
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C75036
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
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TARGET -> AGONIST |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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