dabuzalgron: an alpha(1A/1L)-adrenoceptor partial agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
dabuzalgron : A sulfonamide that is N-phenylmethanesulfonamide which carries a chloro group at position 2, 4,5-dihydro-1H-imidazol-2-ylmethoxy group at position 5, and a methyl group at position 6. Its is a selective alpha-adrenoceptor agonist that is used in the treatment of urinary incontinence. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 216249 |
| CHEMBL ID | 257978 |
| CHEBI ID | 142452 |
| SCHEMBL ID | 5203336 |
| MeSH ID | M0473549 |
| Synonym |
|---|
| ro-115-1240 |
| dabuzalgron [inn] |
| dabuzalgron |
| CHEMBL257978 , |
| CHEBI:142452 |
| dabuzalgronum |
| 219311-44-1 |
| ro 115-1240 |
| n-[6-chloro-3-(4,5-dihydro-1h-imidazol-2-ylmethoxy)-2-methylphenyl]methanesulfonamide |
| unii-lgx4gz74wo |
| lgx4gz74wo , |
| n-(6-chloro-3-((4,5-dihydro-1h-imidazol-2-yl)methoxy)-2-methylphenyl)methanesulfonamide |
| bdbm50377398 |
| gtpl3469 |
| r 450 |
| SCHEMBL5203336 |
| methanesulfonamide, n-(6-chloro-3-((4,5-dihydro-1h-imidazol-2-yl)methoxy)-2-methylphenyl)- |
| n-(6-chloro-3-(4,5-dihydro-1h-imidazol-2-ylmethoxy)-2-methylphenyl)methanesulfonamide |
| AKOS024257909 |
| DTXSID50176345 |
| AS-74067 |
| n-{6-chloro-3-[(4,5-dihydro-1h-imidazol-2-yl)methoxy]-2-methylphenyl}methanesulfonamide |
| Q27076969 |
| ro 115-1240ro 115-1240 |
| CS-0063649 |
| HY-117071 |
| 219311-44-1 (free base) |
| EX-A4502 |
| A911600 |
| Role | Description |
|---|---|
| alpha-adrenergic agonist | An agent that selectively binds to and activates alpha-adrenergic receptors. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| monochlorobenzenes | Any member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine. |
| aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
| sulfonamide | An amide of a sulfonic acid RS(=O)2NR'2. |
| imidazoles | A five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 10.0000 | 0.0008 | 0.3733 | 6.7100 | AID331629 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 10.0000 | 0.0015 | 1.7227 | 5.6000 | AID331627 |
| Alpha-1A adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 0.0250 | 0.0001 | 0.5098 | 7.1000 | AID331623 |
| Alpha-1B adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 10.0000 | 0.0001 | 1.3010 | 5.6000 | AID331625 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID331623 | Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists. |
| AID331627 | Agonist activity at human cloned adrenergic Alpha-1D receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists. |
| AID331625 | Agonist activity at human cloned adrenergic alpha-1B receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists. |
| AID331629 | Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists. |
| AID331624 | Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR relative to phenylephrine | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists. |
| AID1345908 | Human alpha1A-adrenoceptor (Adrenoceptors) | 2004 | BJU international, Jan, Volume: 93, Issue:1 | Pharmacological characteristics of Ro 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist: a potential therapy for stress urinary incontinence. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 6 (100.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (19.91) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (16.67%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (83.33%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||