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| Targets |
Cirazoline primarily targets the α1A-adrenergic receptor, where it acts as a full agonist. It also binds to the α1B and α1D subtypes with lower affinity, functioning as a partial agonist at these receptors. Additionally, cirazoline is a non-selective ligand for imidazoline binding sites. The compound does not exhibit significant activity at other adrenergic receptor subtypes. Its binding affinity (Ki) for the α1A receptor is 120 nM, for the α1B receptor is 960 nM, and for the α1D receptor is 660 nM.
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| ln Vitro |
Cilazoline hydrochloride (5–10 μM; 24 hours) only weakenedly inhibits the GIC death caused by prazosin, without changing GIC survival [1].
Cirazoline acts as a potent full agonist at the α1A-adrenergic receptor. In vitro studies have shown that cirazoline hydrochloride (5-10 μM; 24 hours) only weakly inhibits glioblastoma initiating cell (GIC) death caused by prazosin, without significantly affecting GIC survival. The compound's agonistic activity at α1A-AR leads to the activation of downstream signaling pathways, including the phospholipase C and protein kinase C pathways. |
| ln Vivo |
TST immobility is markedly decreased and neurogenesis is enhanced in mice treated with 40 μM of cilazoline hydrochloride (drinking water) for nine months [1].
In vivo, cirazoline decreases blood pressure when microinjected into the nucleus reticularis lateralis of anesthetized normotensive cats. This effect is mediated through activation of central α1-adrenergic receptors. In mice, treatment with cirazoline hydrochloride at 40 μM in drinking water for nine months markedly decreases TST (tail suspension test) immobility and enhances neurogenesis. This suggests that α1A-AR activation may have antidepressant-like effects. |
| Enzyme Assay |
In vitro receptor binding assays for cirazoline involve measuring the displacement of radiolabeled ligands from adrenergic receptors expressed in cell membranes. Membranes are incubated with [3H]-prazosin or other α1-selective radioligands in the presence of varying concentrations of cirazoline. Bound radioactivity is measured by scintillation counting, and Ki values are calculated from competition binding curves. Selectivity is assessed by testing the compound against a panel of related receptors, including α2-adrenergic and imidazoline binding sites.
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| Cell Assay |
Cell viability assay [1]
Cell Types: glioblastoma Starting cell Tested Concentrations: 5 μM; 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Does not affect GIC cell survival. Cellular assays for cirazoline are performed using cell lines expressing α1-adrenergic receptor subtypes (e.g., HEK293 cells transfected with α1A, α1B, or α1D receptors). Receptor activation is assessed by measuring downstream signaling pathways, such as inositol phosphate accumulation or calcium mobilization using fluorescent indicators. Cells are treated with cirazoline at various concentrations (typically 1 nM to 100 μM), and EC50 values are determined from dose-response curves. These assays confirm the compound's agonist activity and subtype selectivity. |
| Animal Protocol |
Animal/Disease Models: B6/CBA mice [1]
Doses: 40 μM Route of Administration: drinking water; 40 μM; 9-month Experimental Results: Reverse the antidepressant-like phenotype of CAM α1A-AR mice. In vivo animal studies with cirazoline have been performed in cats and mice. In anesthetized cats, cirazoline is microinjected into the nucleus reticularis lateralis, and blood pressure and heart rate are monitored. In mice, cirazoline is administered in drinking water at 40 μM for nine months, and behavioral tests (e.g., tail suspension test) and neurogenesis assays are performed. These studies demonstrate the compound's central nervous system effects and its potential antidepressant-like activity. |
| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for cirazoline are limited. As a research compound, its absorption, distribution, metabolism, and excretion properties have not been extensively characterized. Its molecular weight is 252.74 g/mol. The compound is typically dissolved in suitable solvents for in vitro and in vivo studies. Its lipophilic nature, with a logP of 2.51, suggests moderate membrane permeability. The hydrochloride salt form enhances its aqueous solubility.
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| Toxicity/Toxicokinetics |
Cirazoline is a research compound with limited toxicological data available. It should be handled with standard laboratory safety precautions. No significant adverse effects have been reported in the studies described. The compound's activity at α1-adrenergic receptors could potentially cause cardiovascular effects if administered systemically, including vasoconstriction and hypertension. However, these effects are typically observed at pharmacological doses and are reversible.
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| References |
[1]. Doze VA, et al. alpha(1A)- and alpha(1B)-adrenergic receptors differentially modulate antidepressant-like behaviorin the mouse.Brain Res. 2009 Aug 18;1285:148-57.
[2]. Suzana Assad Kahn , et al. The Anti-Hypertensive Drug Prazosin Inhibits Glioblastoma Growth via the PKCδ-dependent Inhibition of the AKT Pathway. EMBO Mol Med. 2016 May 2;8(5):511-26. |
| Additional Infomation |
Cirazoline HCl is a research compound used as a pharmacological tool to study α1-adrenergic receptor function and imidazoline binding sites. It is particularly valuable for distinguishing between α1A, α1B, and α1D receptor subtypes due to its differential agonist activity. The compound has also been investigated for its potential antidepressant-like effects. It is not approved for clinical use and is intended for laboratory research only.
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| Molecular Formula |
C13H17CLN2O
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|---|---|
| Molecular Weight |
252.74
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| Exact Mass |
252.103
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| CAS # |
40600-13-3
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| Related CAS # |
40600-13-3 (HCl);59939-16-1;
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| PubChem CID |
11957512
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| Appearance |
White to off-white solid powder
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| Density |
1.25g/cm3
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| Boiling Point |
409.5ºC at 760mmHg
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| Flash Point |
201.4ºC
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| LogP |
2.51
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
273
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.C1CN=C(COC2=CC=CC=C2C2CC2)N1
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| InChi Key |
XFRXWLWUUDJHPB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H16N2O.ClH/c1-2-4-12(11(3-1)10-5-6-10)16-9-13-14-7-8-15-13;/h1-4,10H,5-9H2,(H,14,15);1H
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| Chemical Name |
2-[(2-cyclopropylphenoxy)methyl]-4,5-dihydro-1H-imidazole;hydrochloride
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| Synonyms |
Cirazoline HCl; Cirazoline Hydrochloride
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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, 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 : ~33.33 mg/mL (~131.87 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9566 mL | 19.7832 mL | 39.5664 mL | |
| 5 mM | 0.7913 mL | 3.9566 mL | 7.9133 mL | |
| 10 mM | 0.3957 mL | 1.9783 mL | 3.9566 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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