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(OCC2=NCCN2)C=CC(Cl)=C1NS(C)(=O)=O
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 |
|---|---|---|
| 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. | 2009-09 |
|
| A randomized crossover study to evaluate RO 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist in women with stress urinary incontinence. | 2004-06 |
|
| A randomized crossover study to evaluate Ro 115-1240, a selective alpha-adrenoceptor partial agonist in women with stress urinary incontinence. | 2004-05 |
|
| Pharmacological characteristics of Ro 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist: a potential therapy for stress urinary incontinence. | 2004-01 |
|
| A randomized crossover study to evaluate Ro 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist in women with stress urinary incontinence. | 2004-01 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:26:07 GMT 2025
by
admin
on
Mon Mar 31 18:26:07 GMT 2025
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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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Preferred 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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C481520
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CHEMBL257978
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C75036
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SALT/SOLVATE -> PARENT |
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TARGET -> AGONIST |
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ACTIVE MOIETY |
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