MoxonidineI1R/α2AR agonist CAS# 75438-57-2 |
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Quality Control & MSDS
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| Cas No. | 75438-57-2 | SDF | Download SDF |
| PubChem ID | 4810 | Appearance | Powder |
| Formula | C9H12ClN5O | M.Wt | 241.68 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | BDF5895 | ||
| Solubility | DMSO : 20 mg/mL (82.75 mM; Need ultrasonic) | ||
| Chemical Name | 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine | ||
| SMILES | CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC | ||
| Standard InChIKey | WPNJAUFVNXKLIM-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C9H12ClN5O/c1-5-13-7(10)6(8(14-5)16-2)15-9-11-3-4-12-9/h3-4H2,1-2H3,(H2,11,12,15) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
Target: I1-R
Moxonidine is a centrally acting antihypertensive agent. Mixed Nischarin (I1 imidazoline receptor) and α2-AR (adrenergic) agonist; displays 40-fold higher affinity for I1 receptors versus α2-adrenoceptors. Moxonidine reduced stimulated NE overflow (log EC50: -6.15 +/- 0.14). AGN192403, a selective ligand at I1-R, had no influence on the dose-response curve of moxonidine (log EC50: -6.01 +/- 0.25) [1]. The hypotensive and bradycardic actions of moxonidine but not clonidine are mediated through imidazoline receptors and are dependent on intact noradrenergic pathways within the RVLM. Furthermore, the noradrenergic innervation may be associated with a 42 kDa imidazoline receptor protein [2]. References: | |||||
Moxonidine Dilution Calculator
Moxonidine Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.1377 mL | 20.6885 mL | 41.377 mL | 82.7541 mL | 103.4426 mL |
| 5 mM | 0.8275 mL | 4.1377 mL | 8.2754 mL | 16.5508 mL | 20.6885 mL |
| 10 mM | 0.4138 mL | 2.0689 mL | 4.1377 mL | 8.2754 mL | 10.3443 mL |
| 50 mM | 0.0828 mL | 0.4138 mL | 0.8275 mL | 1.6551 mL | 2.0689 mL |
| 100 mM | 0.0414 mL | 0.2069 mL | 0.4138 mL | 0.8275 mL | 1.0344 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Moxonidine is an agonist of I1-imidazoline receptor with EC50 value of 1.3µM [1].
Moxonidine can bind to both I1-imidazoline receptor (I1R) and α2-adrenergic receptor (α2AR). The selectivity of moxonidine for I1R is 33-fold over α2AR. Moxonidine plays its antihypertensive role in the central nervous system. It has a central site of action. It is shown no effect in pithed rats and in cats following spinal cord transaction. Moxonidine also reduces sympathetic outflow and lowers peripheral vascular resistence [1, 2].
Besides the antihypertensive efficacy, Moxonidine is reported to have effects on gastric secretion and gastric mucosal injury in rats. It significantly reduces basal gastric acid secretion when given doses of 0.1 (63% inhibition) and 1.0 (65% inhibition) mg/kg. Even 0.01mg/kg moxonidine can reduce the gastric mucosal injury induced by ethanol [3].
References:
[1] George OK, Gonzalez RR Jr, Edwards LP. Moxonidine, an antihypertensive agent, is permissive to alpha1-adrenergic receptor pathway in the rat-tail artery. J Cardiovasc Pharmacol. 2004 Feb;43(2):306-11.
[2] Morris ST, Reid JL. Moxonidine: a review. J Hum Hypertens. 1997 Oct;11(10):629-35.
[3] Glavin GB, Smyth DD. Effects of the selective I1 imidazoline receptor agonist, moxonidine, on gastric secretion and gastric mucosal injury in rats. Br J Pharmacol. 1995 Feb;114(4):751-4.
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Effect of Moxonidine on the Aldosterone/Renin Ratio in Healthy Male Volunteers.[Pubmed:28324033]
J Clin Endocrinol Metab. 2017 Jun 1;102(6):2039-2043.
Background: The most popular screening test for primary aldosteronism is the plasma aldosterone/renin ratio (ARR). Medications, dietary sodium, posture, and time of day all affect renin and aldosterone levels and can result in false-negative or false-positive ARRs if not controlled. Most antihypertensive medications affect the ARR and can interfere with interpretation of results. To our knowledge, no study has been undertaken to evaluate the effects of Moxonidine on the ARR. Methods: Normotensive, nonmedicated male volunteers (n = 20) underwent measurement (seated, midmorning) of plasma aldosterone (by high-performance liquid chromatography-tandem mass spectrometry), direct renin concentration (DRC), plasma renin activity (PRA), cortisol, electrolytes and creatinine; and urinary aldosterone, cortisol, electrolytes and creatinine at baseline and after 1 week of Moxonidine at 0.2 mg/d and a further 5 weeks at 0.4 mg/d. Results: Compared with baseline, despite the expected significant falls in both systolic and diastolic blood pressure, levels of plasma aldosterone [median, 134 (range, 90 to 535) pmol/L], DRC [20 (10 to 37) mU/L], PRA [2.2 (1.0-3.8) ng/mL/h], and ARR using either DRC [8.0 (4.4 to 14.4)] or PRA [73 (36 to 218)] were not significantly changed after either 1 [135 (98-550) pmol/L, 20 (11-35) mU/L, 2.0 (1.2-4.1) ng/mL/h, 8.8 (4.2 to 15.9), and 73 (32-194), respectively] or 6 weeks [130 (90-500) pmol/L, 22 (8 to 40) mU/L, 2.1 (1.0 to 3.2) ng/mL/h, 7.7 (4.3 to 22.4), and 84 (32 to 192), respectively] of Moxonidine. There were no changes in any urinary measurements. Conclusion: Moxonidine was associated with no significant change in the ARR and may therefore be a good option for maintaining control of hypertension when screening for primary aldosteronism.
[Renoprotecion With Metabolic Syndrome: the Possibility of Receptor Agonist Imidazoline Moxonidine].[Pubmed:28290898]
Kardiologiia. 2016 Oct;56(10):72-79.
The article is devoted to the of prevalence, diagnosis, and prognostic significance of renal damage in metabolic syndrome. The pathogenetic mechanisms of development and progression of chronic kidney disease in individuals with obesity, including the role of increased activity of the sympathetic nervous system is discussed. Approaches to the choice of antihypertensive drugs with an emphasis on metabolic and renal protection properties are given. The advantages of imidazoline receptors in neuroprotective of Moxonidine in patients with arterial hypertension, metabolic syndrome, and diabetes mellitus is discussed in detail. number of mechanisms of renal protection actions of the agonists of imidazoline receptors is described.
Comparison in Conscious Rabbits of the Baroreceptor-Heart Rate Reflex Effects of Chronic Treatment with Rilmenidine, Moxonidine, and Clonidine.[Pubmed:27895591]
Front Physiol. 2016 Nov 15;7:522.
We investigated the effects of chronic subcutaneous treatment with centrally-acting antihypertensive agents Moxonidine, rilmenidine, and clonidine on the baroreflex control of heart rate (HR) in conscious normotensive rabbits over 3 weeks. Infusions of phenylephrine and nitroprusside were performed at week 0 and at weeks 1 and 3 of treatment to determine mean arterial pressure (MAP)-HR baroreflex relationships. A second curve was performed after intravenous methscopolamine to determine the sympathetic baroreflex relationship. The vagal component of the reflex was determined by subtracting the sympathetic curve from the intact curve. Clonidine and Moxonidine (both 1 mg/kg/day), and rilmenidine (5 mg/kg/day), reduced MAP by 13 +/- 3, 15 +/- 2, and 13 +/- 2 mmHg, respectively, but had no effect on HR over the 3-week treatment period. Whilst all three antihypertensive agents shifted baroreflex curves to the left, parallel to the degree of hypotension, Moxonidine and rilmenidine decreased the vagal contribution to the baroreflex by decreasing the HR range of the reflex but Moxonidine also increased sympathetic baroreflex range and sensitivity. By contrast clonidine had little chronic effect on the cardiac baroreflex. The present study shows that second generation agents Moxonidine and rilmenidine but not first generation agent clonidine chronically shift the balance of baroreflex control of HR toward greater sympathetic and lesser vagal influences. These changes if translated to hypertensive subjects, may not be particularly helpful in view of the already reduced vagal contribution in hypertension.
Development of Hydrophilic Interaction Liquid Chromatography Method for the Analysis of Moxonidine and Its Impurities.[Pubmed:27847672]
J Anal Methods Chem. 2016;2016:3715972.
Fast and simple hydrophilic interaction liquid chromatography (HILIC) method was developed and validated for the analysis of Moxonidine and its four impurities (A, B, C, and D) in pharmaceutical dosage form. All experiments were performed on the Agilent Technologies 1200 high-performance liquid chromatography (HPLC) system using Zorbax RX-SIL, 250 mm x 4.6 mm, 5 mum column as stationary phase (T = 25 degrees C, F = 1 mL/min, and lambda = 255 nm), and mixture of acetonitrile and 40 mM ammonium formate buffer (pH 2.8) 80 : 20 (v/v) as mobile phase. Under the optimal chromatographic conditions, selected by central composite design, separation and analysis of Moxonidine and its four impurities are enabled within 12 minutes. Validation of the method was conducted in accordance with ICH guidelines. Based on the obtained results selectivity, linearity (r >/= 0.9976), accuracy (recovery: 93.66%-114.08%), precision (RSD: 0.56%-2.55%), and robustness of the method were confirmed. The obtained values of the limit of detection and quantification revealed that the method can be used for determination of impurities levels below 0.1%. Validated method was applied for determination of Moxonidine and its impurities in commercially available tablet formulation. Obtained results confirmed that validated method is fast, simple, and reliable for analysis of Moxonidine and its impurities in tablets.
