Moxonidine hydrochloride |
| Katalog-Nr.GC11198 |
Moxonidinhydrochlorid ist ein selektiver Agonist am Imidazolinrezeptor Subtyp 1, der als Antihypertensivum verwendet wird.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 75536-04-8
Sample solution is provided at 25 µL, 10mM.
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Moxonidine hydrochloride is a mixed agonist of α2-adrenergic receptor (α2AR) and imidazoline-1 receptor(I1R) with Ki values of 4.2±3.2 nmol/L, 13.0±4.2 nmol/L, 9.5±4.1 nmol/L and 15.6±9.8 nmol/L for I1R, α2AAR, α2BAR andα2CAR, respectively [1].
In multiple acute pain assays, moxonidine has been reported to produce dose-dependent analgesia.In both the α2AAR-dysfunctional and α2CAR-KO experimentsin mice, the rest analgesia function of moxonidine has been revealed to be mediated by α2ARs but not I1Rs [1]. In addition, Moxonidine 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. In bovine adrenal medullary cells, Moxonidine has shown low affinity for I2-relative to I1R sites [2].
References:
[1]Stone LS1, Fairbanks CA, Wilcox GL. Moxonidine, a mixed alpha(2)-adrenergic and imidazoline receptor agonist, identifies a novel adrenergic target for spinal analgesia. Ann N Y Acad Sci. 2003 Dec;1009:378-85.
[2]Ernsberger P1, Damon TH, Graff LM, Schäfer SG, Christen MO.Moxonidine, a centrally acting antihypertensive agent, is a selective ligand for I1-imidazoline sites. J Pharmacol Exp Ther. 1993 Jan;264(1):172-82.
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