Moxonidine is an imidazoline/α-2 receptor agonist used to treat hypertension, especially in cases where ACE inhibitors, β-blockers, calcium channel blockers, and thiazides are not appropriate or provide inadequate blood pressure control. Moxonidine is a new-generation centrally acting antihypertensive drug approved for the treatment of mild to moderate essential hypertension.
- Mechanism
- Curator reviewed · 1 reference
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.
- Primary indication
- For the treatment of mild to moderate essential or primary hypertension.Curator reviewed · 1 structured indication
- Formula / weight
- C9H12ClN5O · 241.677 g/mol (avg)
- Code names
- BDF-5896 · BE 5895 · LY-326869
Resolves to
WPNJAUFVNXKLIM-UHFFFAOYSA-NSMILESCOC1=NC(C)=NC(Cl)=C1NC1=NCCN1What you can answer from here — as of August 30, 2026
Which drugs share a target with Moxonidine, and which of those have an active Phase 3 trial?
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