Moxonidine

Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I₁-R) agonist. Moxonidine activates imidazoline I₁ receptors and α₂ adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis^{[1][2][3][4][5][6][7]}. In Vitro:Moxonidine (10 μM; 48 h) prevents the mild reduction in cardiomyocyte viability/mitochondrial activity induced by IL-1β and TNF-α^[1].
Moxonidine (10 μM; 2 h) increases uptake of oxidised low-density lipoprotein in cultured vascular smooth muscle cells via α2 Adrenoceptors^[2].
Moxonidine (30 μM) inhibits voltage-dependent N-type Ca²⁺ current by activating imidazoline I₁ receptors in rat superior cervical ganglion neurons^[3].
In Vivo:Moxonidine (18 mg/kg/day; p.o.; via drinking water) decreases atherosclerosis formation in the aortic arch and left common carotid artery of ApoE^-/- mice infused with Angiotensin II, associated with increased plasma lipid hydroperoxide levels^[2].
Moxonidine (100-1000 μg/kg; i.v.) causes dose-dependent hypotension and bradycardia in conscious wild-type mice^[4].
Moxonidine (3-6 mg/kg/day; subcutaneous implantation via osmotic minipumps; 21 days) dose-dependently suppresses myocardial infarction-induced sympathetic activation, and the high dose normalizes ventricular weight-body weight ratio and interstitial collagen in rats with myocardial infarction ^[5].
Moxonidine (20-80 nmol; intracerebroventricular injection into the fourth ventricle) dose-dependently lowers mean arterial pressure, heart rate and sympathetic outflow in conscious spontaneously hypertensive rats, with stronger effects than when injected into the lateral ventricle^[6].