Description
Moxonidine hydrochloride is a centrally acting antihypertensive agent. Mixed I1 imidazoline receptor and α2-adrenergic agonist; displays 40-fold higher affinity for I1 receptors versus α2-adrenoceptors.
Moxonidine is a selective high-affinity imidazoline I1-receptor agonist and a selectively low-affinity α2-adrenoceptor agonist. It exhibits anti-hypertensive properties by reducing blood pressure efficiently. Moxonidine also exhibits spinal analgesic activity through the α2C-adrenoceptor component.
Uses
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.
Moxonidine hydrochloride is used as antihypertensive agent. It has been reported to produce dose-dependent analgesia in multiple acute pain assays and has been reported to potently inhibit the binding of [3H]-clonidine to VLM (ventrolateral medulla) membranes in a dose-dependent manner with the IC50 value of 53 ± 10nM.
Application
Moxonidine hydrochloride has been used:
as a standard to study its blood-brain barrier (BBB) permeability in porcine brain lipid extract by parallel artificial membrane permeability assay (PAMPA) method.
as a standard to study the chromatographic behavior and lipophilicity by reversed-phase thin-layer chromatography (RP-TLC).
as an imidazoline I1 receptor agonist to study its effects on excitatory inputs in airway vagal preganglionic neuron (AVPN).
Biological Activity
Moxonidine is a selective high-affinity imidazoline I1-receptor agonist and a selectively low-affinity α2-adrenoceptor agonist. It exhibits anti-hypertensive properties by reducing blood pressure efficiently. Moxonidine also exhibits spinal analgesic activity through the α2C-adrenoceptor component.
