Repositioning Candidate Details
| Candidate ID: | R0492 |
| Source ID: | DB09242 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Moxonidine |
| Synonyms: | |
| Molecular Formula: | C9H12ClN5O |
| SMILES: | COC1=NC(C)=NC(Cl)=C1NC1=NCCN1 |
| Structure: |
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| 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. |
| CAS Number: | 75438-57-2 |
| Molecular Weight: | 241.677 |
| DrugBank Indication: | For the treatment of mild to moderate essential or primary hypertension [L1025]. Effective as most first-line antihypertensives when used as monotherapy [A27137]. |
| 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). [FDA label] |
| 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 [A27150]. 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. [FDA label] 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 [FDA Label]. |
| Targets: | Alpha-2A adrenergic receptor; Nischarin |
| Inclusion Criteria: |
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