| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
α adrenergic receptor
Idazoxan HCl targets α2-adrenoceptors (α2A, α2B, and α2C) and imidazoline receptors (I1 and I2). It is an antagonist at α2-adrenoceptors and imidazoline receptors. Idazoxan is an antagonist at I1 imidazoline binding sites and an I2 imidazoline binding site ligand. The pKi values are 5.90 for I1, 7.22 for I2, 8.01 for α2A, 7.43 for α2B, and 7.7 for α2C receptors. Idazoxan has moderate affinity for the 5-HT1A receptors. |
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| ln Vitro |
The central hypotensive effect of imidazoline-like drugs (IMs) involves non-adrenergic imidazoline receptors (IRs). IMs cause hypotension irrespective of their affinity and selectivity for one or the other α-adrenoceptor subtypes. LNP 509, which binds to I1Rs (Ki= 5.10−7 M) but roughly not to α2-adrenoceptors (A2Rs) (Ki >10−5 M), causes hypotension when injected alone into the brainstem. As far as hybrid drugs, that is, those with mixed binding profiles (I1/α2), are concerned, a significant correlation was reported between their central hypotensive effect and their affinity for IRs. Imidazoline antagonists such as Idazoxan competitively antagonized the centrally induced hypotensive effect of IMs. Yohimbine, an A2Rs antagonist, blocks the hypotensive effect of hybrids but usually in a noncompetitive manner. Mutation of A2Rs prevented the hypotensive effects of drugs highly selective for A2Rs, but also that of hybrids such as clonidine. These data indicate that triggering of the hypotensive effects of IMs (1) needs implication of IRs; (2) appears to be facilitated by additional activation of A2Rs; and (3) requires integrity of A2Rs along the sympathetic pathways[2].
In vitro, idazoxan inhibits the forskolin-stimulated adenylate cyclase activity to the same extent as 5-HT in the rat hippocampus. The compound has moderate affinity for the 5-HT1A receptors. Idazoxan is an antagonist at α2-adrenoceptors and imidazoline receptors. The compound's binding affinity for various receptors has been characterized using radioligand binding assays. |
| ln Vivo |
Idazoxan HCl (RX781094A; RX-781094 hydrochloride) is a potent and selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor. Idazoxan has not been brought to market as an antidepressant for the treatment of schizophrenia, although it has been studied for this purpose.
1. Idazoxan (1, 3, 10 mg kg-1, i.p.) produced a significant increase in food and water intake in freely feeding rats during the daylight phase. 2. The more selective and specific alpha 2-adrenoceptor antagonists, RX811059 (0.3, 1, 3 mg kg-1, i.p.) and RX821002 (0.3, 1, 3 mg kg-1, i.p.), did not produce hyperphagia in rats, however, the highest dose produced a significant increase in water intake. 3. The peripherally acting alpha 2-adrenoceptor antagonist, L-659,066 (1, 3, 10 mg kg-1, i.p.), did not affect food intake in the 4 h following injection, but the highest dose (10 mg kg-1), produced a large increase in water intake. 4. These results indicate that alpha 2-adrenoceptor antagonists may increase water intake by a peripherally mediated mechanism. 5. The lack of effect RX811059 and RX821002 on food intake contrasts with the large dose-related increases induced by idazoxan and suggests that the hyperphagic effects of idazoxan are not due to alpha 2-adrenoceptor blockade but may instead reflect its affinity for a non-adrenoceptor site, a property not shared by the other alpha 2-antagonists[1]. In vivo, idazoxan has been studied as a potential antidepressant for the treatment of schizophrenia, but it has not yet entered the market. The compound's effects on metabolism, secretion, ion transport, and cardiovascular/cerebrovascular function have been investigated. Idazoxan's antagonism of α2-adrenoceptors and imidazoline receptors contributes to its pharmacological effects. Further clinical studies are needed to establish its efficacy and safety. |
| Enzyme Assay |
The pharmacological properties of Idazoxan, 2-[2-(1,4-benzodioxanyl)]-2-imidazoline, were first described four years ago; since then, this compound has been revealed to be one of the most selective alpha 2-adrenoceptor blocking agent presently available. At peripheral sites, idazoxan antagonized the effects of alpha 2 agonists such as azepexole, B-HT 920, M 7, UK 14,304, alpha-methylnoradrenaline, clonidine but was ineffective against alpha 1 agonists such as cirazoline and phenylephrine. At presynaptic sites idazoxan increased the tachycardia due to the stimulation of the cardioaccelerator nerve of the dog and antagonized the inhibitory effects of alpha 2 agonists in dogs and rats. As compared to the classical alpha 2-adrenoceptor blocking agents, idazoxan was more selective and as potent as yohimbine, rauwolscine, RS 21361, Wy 26703. At central sites, idazoxan has been found to antagonize the sympathoinhibitory effects of alpha 2 agonists. Therefore, idazoxan is a potent and probably the most selective alpha 2-adrenoceptor blocking agent presently available and is now frequently used for the investigation of peripheral and central alpha 2-adrenoceptors.[3]
In vitro receptor binding assays for idazoxan HCl involve measuring its binding affinity to α2-adrenoceptors and imidazoline receptors. The receptor is incubated with a radiolabeled ligand and varying concentrations of idazoxan. The displacement of the radiolabeled ligand is measured, and the IC50 or Ki value is calculated. The compound's functional activity is assessed using cAMP accumulation assays or other second messenger assays. |
| Cell Assay |
In vitro cell-based assays for idazoxan HCl evaluate its effects on receptor-mediated signaling. Cells expressing α2-adrenoceptors or imidazoline receptors are treated with idazoxan, and the inhibition of agonist-induced signaling is measured. cAMP levels are measured using ELISA or radioimmunoassay. The compound's effects on cell proliferation and apoptosis are assessed using MTT or flow cytometry.
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| Animal Protocol |
Male CD-COBS rats injected with 1 mg/kg haloperidol
0.16 mg/kg, 0.31 mg/kg, 0.63 mg/kg, 1.25 mg/kg, 2.5 mg/kg, and 5.0 mg/kg Subcutaneous injection; for 1 hour In vivo, idazoxan HCl is evaluated in animal models of neurological and psychiatric disorders. The compound is administered via various routes, and behavioral, physiological, and biochemical endpoints are assessed. The compound's effects on depression, anxiety, and cognition are evaluated using behavioral tests. Pharmacokinetic studies are conducted to determine the compound's absorption, distribution, metabolism, and excretion. |
| ADME/Pharmacokinetics |
Idazoxan HCl (RX 781094 hydrochloride) is a potent and selective α2 adrenergic receptor antagonist and an antagonist for the imidazoline receptor. It has a molecular formula of C₁₁H₁₃ClN₂O₂ and a molecular weight of 240.69 g/mol. Idazoxan HCl is soluble in water and DMSO. The compound should be stored at room temperature. It is for research use only.
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| Toxicity/Toxicokinetics |
The oral LD50 in mice was 85 mg/kg. (European Journal of Medicinal Chemistry – Therapeutic Chemistry, 25(557), 1990)
The toxicity of idazoxan HCl has been evaluated in preclinical studies. The compound has shown a favorable safety profile at therapeutic doses. In animal studies, idazoxan has been well-tolerated, with no significant adverse effects reported at doses that provide pharmacological effects. The compound's safety in humans has not been extensively studied, and further clinical trials are needed to establish its safety and efficacy. |
| References |
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| Additional Infomation |
benzodioxane-linked imidazole compound with α-2 adrenergic receptor antagonistic activity.
See also: Idazoline (note moved to). Idazoxan HCl (RX 781094 hydrochloride) is a benzodioxane-linked imidazoline compound that functions as an antagonist at α2-adrenoceptors and imidazoline receptors (IRs). It is a potent and selective α2 adrenergic receptor antagonist. Idazoxan HCl is also an antagonist for the imidazoline receptor. It has been studied as a potential antidepressant for the treatment of schizophrenia but has not yet entered the market. |
| Molecular Formula |
C11H13CLN2O2
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|---|---|
| Molecular Weight |
240.686
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| Exact Mass |
240.067
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| Elemental Analysis |
C, 54.89; H, 5.44; Cl, 14.73; N, 11.64; O, 13.29
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| CAS # |
79944-56-2
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| Related CAS # |
79944-56-2 (HCl); 79944-58-4
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| PubChem CID |
154494
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| Appearance |
White to off-white solid powder
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| Boiling Point |
397ºC at 760 mmHg
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| Flash Point |
193.9ºC
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| LogP |
1.394
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
267
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.N1CCNC=1C1COC2C(=CC=CC=2)O1
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| InChi Key |
MYUBYOVCLMEAOH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H12N2O2.ClH/c1-2-4-9-8(3-1)14-7-10(15-9)11-12-5-6-13-11;/h1-4,10H,5-7H2,(H,12,13);1H
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| Chemical Name |
2-(2,3-dihydro-1,4-benzodioxin-3-yl)-4,5-dihydro-1H-imidazole;hydrochloride
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| Synonyms |
RX-781094A; RX781094A; RX781094; IDAZOXAN HYDROCHLORIDE; 79944-56-2; Idazoxan (hydrochloride); Idazoxan HCl; (+/-)-Idazoxan Monohydrochloride; 2-(2,3-Dihydrobenzo[b][1,4]dioxin-2-yl)-4,5-dihydro-1H-imidazole hydrochloride; MLS000069708; RX 781094A; RX 781094; Idazoxan HCl; RX-781094; Idazoxan 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) |
DMSO: ~125 mg/mL (~519.3 mM)
H2O: ~100 mg/mL (~415.5 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.64 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 20.8 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: ≥ 2.08 mg/mL (8.64 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 20.8 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: ≥ 2.08 mg/mL (8.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (207.74 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1547 mL | 20.7736 mL | 41.5472 mL | |
| 5 mM | 0.8309 mL | 4.1547 mL | 8.3094 mL | |
| 10 mM | 0.4155 mL | 2.0774 mL | 4.1547 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05727189 | Recruiting | Drug: TR-01-XRS Drug: TR-01-XR Drug: TR-01-IR |
Healthy | Terran Biosciences Australia Pty Ltd |
February 14, 2023 | Phase 1 |
Products are for research use only; We do not sell to patients
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