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Moxonidine is an imidazoline 1 (I1) receptor agonist (Ki = 56 nM in a radioligand binding assay).1 It is also an agonist of the α2A-adrenergic receptor (α2A-AR; Ki = 150 nM in a radioligand binding assay). It is selective for I1 and α2A-AR receptors over α1-, α2B, and α2C-ARs (Kis = >30,000, 1,000, and 2,000 nM, respectively). Moxonidine decreases mean arterial pressure in spontaneously hypertensive rats when administered at a dose of 0.2 nmol injected into the rostral ventrolateral medulla oblongata (RVLM).2 It also reduces blood pressure in cynomolgus monkeys when administered at a dose of 167 µg/kg.1
WARNING This product is not for human or veterinary use.
1. Synthesis and pharmacologic evaluation of 2-
2. A novel mechanism of action for hypertension control: moxonidine as a selective I1-