| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Alpha-adrenergic receptors and imidazoline receptors. Tolonidine is an imidazoline receptor agonist and alpha-adrenergic receptor agonist.
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|---|---|
| ln Vitro |
In vitro, Tolonidine is characterized as an imidazoline receptor agonist and alpha-adrenergic receptor agonist. It is structurally related to clonidine.
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| ln Vivo |
Intravenous tolonidine reduces peripheral vascular resistance, lowers aortic blood flow, and decreases the amplitude of ventricular contractions in dogs under anesthesia [1]. Tolonidine generates a sustained rise in blood pressure without subsequent hypotension in doubly denervated rats, indicating that it may have peripheral sympathomimetic effects [1].
In vivo, Tolonidine is orally bioavailable and has hypotensive and anti-hypertensive effects. Intravenous tolonidine reduces peripheral vascular resistance, lowers aortic blood flow, and decreases the amplitude of ventricular contractions in anesthetized dogs. It shows efficacy in lowering blood pressure by reducing vascular resistance and heart rate. |
| Enzyme Assay |
Non-cell receptor binding assays for Tolonidine are performed using membrane preparations from tissues expressing alpha-adrenergic or imidazoline receptors. Radioligand binding studies are conducted using [³H]clonidine or [³H]idazoxan as tracers. Membranes are incubated with the radioligand and varying concentrations of Tolonidine (0.001-100 μM). Nonspecific binding is determined with excess unlabeled clonidine or idazoxan. After incubation at 25°C for 60 minutes, bound and free ligand are separated by filtration, and radioactivity is counted. Ki values are calculated from competition curves.
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| Cell Assay |
Cellular assays for Tolonidine are performed using cells expressing alpha-adrenergic receptors or imidazoline receptors. Cells are treated with Tolonidine at concentrations ranging from 0.01-100 μM. Receptor activation is measured by inhibition of forskolin-stimulated cAMP accumulation (for alpha-2 receptors) or by calcium mobilization. EC₅₀ values for receptor activation are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies are conducted in rodent or canine models. Tolonidine is administered intravenously or orally at doses determined from pharmacokinetic studies. Blood pressure, heart rate, and peripheral vascular resistance are measured. Aortic blood flow and ventricular contraction amplitude are assessed. The compound's antihypertensive efficacy is evaluated.
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| ADME/Pharmacokinetics |
Tolonidine has a molecular weight of 209.68 and a molecular formula of C10H12ClN3. It is orally bioavailable. The compound is an imidazoline receptor agonist and alpha-adrenergic receptor agonist.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Tolonidine are limited. As a centrally acting antihypertensive agent, potential adverse effects may include sedation, dry mouth, and bradycardia. No significant organ-specific toxicity has been reported at effective doses.
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| References |
[1]. Pharmacological properties of 2-(2-chloro-p-toluidino)-2-imidazoline-nitrate (tolonidine), a new antihypertensive agent. II. Action on cardiac contraction, circulatory parameters, autonomic receptors and diuresis. Arzneimittelforschung. 1975 Nov;25(11):1802-6.
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| Additional Infomation |
Tolonidine is a substituted aniline.
Tolonidine is a centrally acting antihypertensive agent. It is an imidazoline receptor agonist and alpha-adrenergic receptor agonist. Structurally related to clonidine, it lowers blood pressure by reducing vascular resistance. Tolonidine is not approved for clinical use in most countries. |
| Molecular Formula |
C10H12CLN3
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|---|---|
| Molecular Weight |
209.67
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| Exact Mass |
209.072
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| Elemental Analysis |
C, 57.28; H, 5.77; Cl, 16.91; N, 20.04
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| CAS # |
4201-22-3
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| Related CAS # |
4201-22-3;57524-15-9 (nitrate);
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| PubChem CID |
72138
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| Appearance |
White to off-white solid powder
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| Density |
1.31g/cm3
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| Boiling Point |
314ºC at 760 mmHg
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| Flash Point |
143.7ºC
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| Index of Refraction |
1.637
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| LogP |
1.856
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
229
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=C(C=C1)NC2=NCCN2)Cl
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| InChi Key |
KWBTZIFLQYYPTH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H12ClN3/c1-7-2-3-9(8(11)6-7)14-10-12-4-5-13-10/h2-3,6H,4-5H2,1H3,(H2,12,13,14)
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| Chemical Name |
N-(2-chloro-4-methylphenyl)-4,5-dihydro-1H-imidazol-2-amine
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| Synonyms |
ST-375; Euctan; ST 375; ST375;4201-22-3; Tolonidina; N-(2-chloro-4-methylphenyl)-4,5-dihydro-1H-imidazol-2-amine; Tolonidinum; Tolonidine
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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 |
| 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) |
DMSO : ~100 mg/mL (~476.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.92 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (11.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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: ≥ 2.5 mg/mL (11.92 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 | 4.7694 mL | 23.8470 mL | 47.6940 mL | |
| 5 mM | 0.9539 mL | 4.7694 mL | 9.5388 mL | |
| 10 mM | 0.4769 mL | 2.3847 mL | 4.7694 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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