Investigational Drug Details
Drug ID: | D232 |
Drug Name: | Moxonidine |
Synonyms: | (2R,4R)-1-[(2S)-5-[(aminoiminomethyl)amino]-1-oxo-2-[[(1,2,3,4-tetrahydro-3-methyl-8- quinolinyl)sulfonyl]amino]pentyl]-4-methyl-2-piperidinecarboxylic acid; Moxonidine |
Type: | Chemical drug |
DrugBank ID: | DB09242 |
DrugBank Description: | Moxonidine is a new-generation centrally acting antihypertensive drug approved for the treatment of mild to moderate essential hypertension. It is suggested to be effective in cases where other agents such as thiazides, beta-blockers, ACE inhibitors, and calcium channel blockers are not appropriate or irresponsive. As well, moxonidine has been shown to present blood pressure-independent beneficial effects on insulin resistance syndrome. |
PubChem ID: | 4810 |
CasNo: | 75438-57-2 |
Repositioning for NAFLD: | Yes |
SMILES: | N(c1c(OC)nc(nc1Cl)C)C1=NCCN1 |
Structure: |
|
InChiKey: | WPNJAUFVNXKLIM-UHFFFAOYSA-N |
Molecular Weight: | 241.682 |
DrugBank Targets: | Alpha-2A adrenergic receptor agonist; Nischarin agonist |
DrugBank MoA: | Stimulation of central alpha 2-adrenergic receptors is associated with sympathoadrenal suppression and subsequent reduction of blood pressure. As this class was further explored it was discovered that sympathoadrenal activity can also be suppressed by a second pathway with a newly discovered drug target specific to imidazolines . Specifically, moxonidine binds the imidazoline receptor subtype 1 (I1) and to a lesser extent αlpha-2-adrenoreceptors in the RSV causing a reduction of sympathetic activity, reducing systemic vascular resistance and thus arterial blood pressure. Moreover, since alpha-2-adrenergic receptors are considered the primary molecular target that facilitates the most common side effects of sedation and dry mouth that are elicited by most centrally acting antihypertensives, moxonidine differs from these other centrally acting antihypertensives by demonstrating only low affinity for central alpha-2-adrenoceptors compared to the aforementioned I1-imidazoline receptors . |
DrugBank Pharmacology: | Antihypertensive agent whose site of action is the Central Nervous System (CNS), specifically involving interactions with I1- imidazoline and alpha-2-adrenergic rececptors within the rostral ventrolateral medulla (RSV). |
DrugBank Indication: | For the treatment of mild to moderate essential or primary hypertension . Effective as most first-line antihypertensives when used as monotherapy . |
Targets: | NISCH agonist |
Therapeutic Category: | -- |
Clinical Trial Progress: | Phase 4 on-going (ACTRN12617000948392) |
Latest Progress: | Under clinical trials |

Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
---|---|---|---|---|---|---|---|
L0995 | ACTRN12617000948392 | Phase 4 | Not yet recruiting | -- | 3/07/2017 | 3/07/2017 | Details |
Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
---|
Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
---|---|---|---|---|---|
S01 | Improve insulin resistance | insulin sensitizer; insulin resistance; glucose tolerance | Biguanide: increases 5-AMP activated protein kinase signaling; SGLT-2 inhibitor; Thiazalidinedione: selective PPAR-γ agonists; GLP-1 agonist | Metformin; Empagliflozin; Canagliflozin; Rosiglitazone; Pioglitazone; Liraglutide | Details |
Article ID | PMID | Source | Title | |
---|---|---|---|---|
A02990 | 34171957 | Vnitr Lek | The use of moxonidine in the treatment of arterial hypertension. | Details |
A53139 | 10842668 | Ann N Y Acad Sci | Molecular pathology in the obese spontaneous hypertensive Koletsky rat: a model of syndrome X. | Details |
A53147 | 10321453 | Blood Press Suppl | Anti-hyperglycemic activity of moxonidine: metabolic and molecular effects in obese spontaneously hypertensive rats. | Details |