| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
mGluR5
AZD 2066 hydrate is a selective antagonist targeting the metabotropic glutamate receptor 5 (mGluR5), which is a G protein-coupled receptor involved in glutamatergic signaling in the central nervous system. It also activates the BDNF/trkB signaling pathway as part of its downstream mechanism. The compound is selective for mGluR5 and does not significantly interact with other mGlu receptor subtypes based on its selective antagonist profile. |
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| ln Vitro |
AZD 2066 (one to ten micrograms) suppresses the calcium response in mGlu5/HEK cells, striatal, hippocampal, and cortical cultures, with IC50s of 27.2±9.1, 3.56±0.52, 96.2±17.8, and 380±78.0 nM, respectively[2]. In mGlu5/HEK cells, AZD 2066 (1–10 μM) abolishes Quis's effects and the rhythmic Ca2+ response brought on by DHPG administration in a bath[2]. Striatal neurons respond less favorably to AZD 2066(1–10 μM)[2].
In vitro, AZD 2066 inhibits Ca2+ response in a concentration-dependent manner (1-10 microM), with IC50 values of 27.2+/-9.1 nM in mGlu5/HEK cells, 3.56+/-0.52 nM in striatal cultures, 96.2+/-17.8 nM in hippocampal cultures, and 380+/-78.0 nM in cortical cultures. It also inhibits oscillatory Ca2+ responses induced by DHPG and blocks the effects of either DHPG or Quis in mGlu5/HEK cells, while striatal neurons are less responsive. |
| ln Vivo |
In rats, AZD 2066 (0.03-30 mg/kg; po) demonstrates discriminative effects[1].
In vivo, AZD 2066 (0.03-30 mg/kg; p.o.) shows discriminative effects in male Wistar rats (weighing 240-250 g), causing full and dose-dependent AZD9272-appropriate responding 60 minutes after administration. At 5 mg/kg (i.p., 2 × 12 h), it alleviates chronic social defeat stress-induced depressive behaviors in mice. At 10 microM via brain slide perfusion, it alleviates DHPG-facilitated long-term depression expression in CSDS-treated mice via BDNF/trkB signaling. |
| Enzyme Assay |
For AZD 2066 hydrate, mGluR5 binding affinity is assessed using radioligand binding assays with membrane preparations from cells expressing recombinant human mGluR5. Varying concentrations of the test compound are incubated with a specific mGluR5 radioligand. Non-specific binding is determined in the presence of a reference antagonist. The reaction mixture is filtered and washed, and bound radioactivity is measured using a scintillation counter to calculate IC50 or Ki values.
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| Cell Assay |
For AZD 2066 hydrate, mGlu5/HEK cells or primary neuronal cultures (striatal, hippocampal, cortical) are loaded with a calcium-sensitive fluorescent dye (e.g., Fluo-4 or Fura-2). Cells are pre-incubated with varying concentrations of AZD 2066 (1-10 microM) before stimulation with an mGluR5 agonist (e.g., DHPG or Quis). Fluorescence intensity (reflecting intracellular Ca2+) is measured using a fluorescence plate reader or microscope, and IC50 values are calculated.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats (weighing 240-250 g)[1]
Doses: 0.03, 0.1, 0.3, 1, 3, 10 , 30 mg/kg Route of Administration: Po (60 minutes after administration) Experimental Results: Caused full and dose-dependent AZD9272-appropriate responding. For AZD 2066 hydrate, male Wistar rats (240-250 g) are dosed orally with AZD 2066 (0.03, 0.1, 0.3, 1, 3, 10, 30 mg/kg). Responding is assessed 60 minutes after administration to evaluate discriminative effects. In mouse depressive models (C57BL/6 mice subjected to CSDS), AZD-2066 is administered intraperitoneally at 5 mg/kg (2 × 12 h) to assess alleviation of depressive behaviors. Brain slice perfusion at 10 microM is used to evaluate LTD expression via BDNF/trkB signaling. |
| ADME/Pharmacokinetics |
AZD 2066 hydrate is characterized as orally active and blood-brain barrier-permeating, indicating good oral bioavailability and CNS penetration. The compound shows discriminative effects in rats at doses ranging from 0.03-30 mg/kg (p.o.), demonstrating dose-dependent systemic exposure. Metabolic stability and drug-drug interaction potential have been assessed using in vitro metabolism tools and PBPK modeling, with no significant interaction predicted for most CYP enzymes except CYP3A4.
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| Toxicity/Toxicokinetics |
Available literature does not provide detailed toxicology data for AZD 2066 hydrate. As a research compound, routine safety assessments for acute toxicity, genotoxicity, and organ-specific toxicity have not been described in product documentation. For laboratory use, standard chemical safety precautions are recommended. In clinical development, AstraZeneca discontinued development for undisclosed reasons, which may include safety or efficacy considerations.
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| References |
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| Additional Infomation |
AZD 2066 hydrate was previously under development by AstraZeneca for oral treatment of pain indications (chronic neuropathic pain, painful diabetic neuropathies), depressive disorders, and gastroesophageal reflux disease. The hydrochloride salt form is also available. The compound activates the BDNF/trkB signaling pathway as part of its mechanism. Development may have been discontinued for undisclosed reasons. It is available as a research tool for studying mGluR5 biology and associated CNS disorders.
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| Molecular Formula |
C19H16CLN5O2.1/4H2O
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| Molecular Weight |
386.33
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| Related CAS # |
AZD 2066;934282-55-0
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| Appearance |
Off-white to light yellow solid powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.5885 mL | 12.9423 mL | 25.8846 mL | |
| 5 mM | 0.5177 mL | 2.5885 mL | 5.1769 mL | |
| 10 mM | 0.2588 mL | 1.2942 mL | 2.5885 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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