| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Rilmenidine acts as a selective agonist at imidazoline receptors (particularly the I1 subtype) and also as an agonist at alpha2-adrenergic receptors. Its central hypotensive activity is mediated by stimulation of alpha2 adrenoceptors in the region of the nucleus tractus solitarii, the vasomotor center, and the nucleus of the vagus nerve. Rilmenidine binds to imidazoline receptors in bovine rostral ventrolateral medulla homogenates with a Ki of 6.1 nM, and to alpha2-adrenergic receptors in bovine prefrontal cortex homogenates with a Ki of 87 nM. The drug decreases sympathetic tone mainly by an action on the adrenal medulla.
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| ln Vitro |
The effectiveness of rimedine as an antihypertensive is similar to that of angiotensin-converting enzyme (ACE) inhibitors, beta-blockers, calcium channel blockers, and diuretics [1]. The growth of K562 cells is inhibited by rilmenidine (25–100 μM; 24 hours) [2].
In radioligand binding studies, rilmenidine demonstrates somewhat higher selectivity for alpha2 adrenoceptors, though this selectivity is not reflected by a clearly different pharmacologic profile. The compound effectively decreases plasma noradrenaline and adrenaline levels and corrects the decrease in leukocyte beta-adrenoceptors. Rilmenidine (25-100 μM) shows activity in various in vitro systems. As an imidazoline receptor agonist, it activates I1 receptors which are involved in the central regulation of sympathetic outflow. |
| ln Vivo |
N171-82Q mice treated with rilmenidine (ip; 4 times per week) demonstrated significant gains in forelimb grip strength and all limb grip strength between 12 and 22 weeks of age [3]. Rilmenidine decreases levels of mutant huntingtin protein [3].
Rilmenidine effectively lowers blood pressure in various animal models. In spontaneously hypertensive rats, rilmenidine is effective and potent as an antihypertensive agent. In anesthetized rats, rilmenidine induces hypotension and bradycardia with ED50 values of 0.25 and 0.35 mg/kg, respectively. It also reduces mean arterial pressure and renal sympathetic nerve activity. The compound decreases sympathetic tone mainly by an action on the adrenal medulla. Its ability to lower blood pressure in sympathetically denervated dogs indicates additional peripheral effects. |
| Enzyme Assay |
Receptor binding assays for rilmenidine are performed using membrane homogenates from tissues expressing imidazoline receptors (e.g., bovine rostral ventrolateral medulla) or alpha2-adrenergic receptors (e.g., bovine prefrontal cortex). Radioligand binding studies utilize appropriate tracers such as [3H]-clonidine or [3H]-idazoxan for imidazoline receptors. Membranes are incubated with varying concentrations of rilmenidine and fixed radioligand in binding buffer for 60 minutes at room temperature. Non-specific binding is determined in the presence of excess unlabeled ligand. Bound radioligand is separated by rapid filtration and counted. Ki values are calculated from competition curves.
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| Cell Assay |
Cell viability assay [2]
Cell Types: K562 Cell Tested Concentrations: 25, 50, 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dose-dependent inhibition of K562 colony formation. Functional cellular assays for imidazoline or alpha2-adrenergic receptor activity typically employ cell lines expressing the respective receptors. For alpha2-adrenergic receptor activity, cells are treated with rilmenidine and downstream signaling (e.g., inhibition of cAMP accumulation) is measured. For imidazoline receptor studies, cells expressing I1 receptors are used to assess receptor activation and signaling. The effects of rilmenidine on autophagy can be studied in various cell lines by monitoring LC3-II accumulation and autophagosome formation. |
| Animal Protocol |
In vivo efficacy is evaluated in hypertensive animal models including spontaneously hypertensive rats and renal hypertensive models. Blood pressure is measured via tail-cuff plethysmography or telemetry. Rilmenidine is administered orally or intravenously at various doses. The antihypertensive effect is monitored over time, with measurement of heart rate and other cardiovascular parameters. In sympathetically denervated dogs, the ability of rilmenidine to lower blood pressure is assessed to determine the contribution of central versus peripheral mechanisms.
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| ADME/Pharmacokinetics |
Rilmenidine is orally active and rapidly absorbed following oral administration. As an antihypertensive agent, it is typically administered once or twice daily. The compound has a favorable pharmacokinetic profile with good oral bioavailability. Rilmenidine hemifumarate has molecular formula C24H36N4O6 and molecular weight 476.57. The compound's pharmacokinetics support its use as a once-daily antihypertensive agent.
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| Toxicity/Toxicokinetics |
Common adverse effects of rilmenidine are related to its central alpha2-adrenergic agonist activity and may include sedation, dry mouth, dizziness, and fatigue. Compared to older alpha2 agonists like clonidine, rilmenidine has a more favorable side effect profile due to its selectivity for imidazoline receptors over alpha2-adrenergic receptors. The compound should be used with caution in patients with severe renal impairment. As with other centrally acting antihypertensives, abrupt discontinuation may lead to rebound hypertension.
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| References | |
| Additional Infomation |
Rilmenidine is approved as an antihypertensive agent in several countries. It is also known as S-3341 and oxaminozoline. Beyond its antihypertensive use, rilmenidine has been investigated for its ability to induce autophagy, which may have implications for neuroprotection and longevity research. The compound's dual action at imidazoline and alpha2-adrenergic receptors makes it a valuable tool for studying the role of these receptors in cardiovascular regulation.
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| Molecular Formula |
C24H36N4O6
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| Molecular Weight |
476.565846443176
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| Exact Mass |
476.263
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| CAS # |
207572-68-7
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| Related CAS # |
Rilmenidine;54187-04-1
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| PubChem CID |
45073450
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
338
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC1C(C2CC2)NC3=NCCO3.C1CC1C(C2CC2)NC3=NCCO3.C(=C/C(=O)O)\C(=O)O
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| InChi Key |
LZFATBMLSYHRTC-WXXKFALUSA-N
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| InChi Code |
InChI=1S/2C10H16N2O.C4H4O4/c2*1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10;5-3(6)1-2-4(7)8/h2*7-9H,1-6H2,(H,11,12);1-2H,(H,5,6)(H,7,8)/b;;2-1+
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| Chemical Name |
(E)-but-2-enedioic acid;N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~209.84 mM)
DMSO : ~10 mg/mL (~41.97 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1 mg/mL (4.20 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0983 mL | 10.4916 mL | 20.9833 mL | |
| 5 mM | 0.4197 mL | 2.0983 mL | 4.1967 mL | |
| 10 mM | 0.2098 mL | 1.0492 mL | 2.0983 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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