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Purity: ≥98%
AZD-8529 is a novel, potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2 (group II metabotropic glutamate receptors) with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes. AZD8529 enhanced agonist-induced mGluR2 activation in primate cortex, hippocampus, and striatum as well as in the membrane-binding assay. At doses (.3–3 mg/kg) that had no effect on food self-administration, AZD8529 reduced the self-administration of nicotine in monkeys. Additionally, AZD8529 lessened the recurrence of nicotine priming and cue-induced nicotine seeking following the cessation of drug-reinforced responding. AZD8529 reduced the release of dopamine induced by nicotine in the accumbens in rats.
| Targets |
mGluR2 ( EC50 = 285 nM )
|
|---|---|
| ln Vitro |
AZD-8529 increases the effects of glutamate at mGluR2 with an EC50 of 195 nM [1].
AZD-8529 does not cause antagonist reactions on mGluRs at 25 μM[1]. |
| ln Vivo |
AZD-8529 (0.3-mg/kg, i.m.) AZD-8529 mesylate (0.3 mg/kg, i.m.) lessens cue- and priming-induced reinstatement in squirrel monkeys[1].
AZD-8529 (30 mg/kg; i.p.) reduces the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats[1]. |
| Animal Protocol |
Sprague-Dawley rats
10 mg/kg, 30 mg/kg Intraperitoneal injection; 2 hours before nicotine injections |
| References |
| Molecular Formula |
C24H24F3N5O3
|
|---|---|
| Molecular Weight |
487.474275588989
|
| Exact Mass |
487.18
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| Elemental Analysis |
C, 59.13; H, 4.96; F, 11.69; N, 14.37; O, 9.85
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| CAS # |
1092453-15-0
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| Related CAS # |
AZD-8529 mesylate; 1314217-69-0
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| Appearance |
Solid powder
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| SMILES |
CC1=CC(=CC2=C1C(=O)N(C2)CC3=CC=C(C=C3)OC(F)(F)F)C4=NC(=NO4)CN5CCNCC5
|
| InChi Key |
IPCYZQQFECEHLI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H24F3N5O3/c1-15-10-17(22-29-20(30-35-22)14-31-8-6-28-7-9-31)11-18-13-32(23(33)21(15)18)12-16-2-4-19(5-3-16)34-24(25,26)27/h2-5,10-11,28H,6-9,12-14H2,1H3
|
| Chemical Name |
7-methyl-5-[3-(piperazin-1-ylmethyl)-1,2,4-oxadiazol-5-yl]-2-[[4-(trifluoromethoxy)phenyl]methyl]-3H-isoindol-1-one
|
| Synonyms |
AZD8529; AZD-8529; AZD 8529
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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)
|
| Solubility (In Vitro) |
DMSO: ~128.2 mg/mL (~71.4 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (12.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 62.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0514 mL | 10.2570 mL | 20.5141 mL | |
| 5 mM | 0.4103 mL | 2.0514 mL | 4.1028 mL | |
| 10 mM | 0.2051 mL | 1.0257 mL | 2.0514 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 |
| NCT00755378 | Completed | Drug: AZD8529 Drug: Placebo |
Healthy Volunteer | AstraZeneca | September 2008 | Phase 1 |
| NCT00765492 | Completed | Drug: AZD8529 Drug: Placebo |
Healthy Volunteer | AstraZeneca | October 2008 | Phase 1 |
| NCT00886756 | Completed | Drug: AZD8529 Drug: Placebo |
Healthy | AstraZeneca | April 2009 | Phase 1 |
| NCT02401022 | Completed | Drug: AZD8529 | Tobacco Use Disorder | National Institute on Drug Abuse (NIDA) |
July 2015 | Phase 2 |
| NCT00921804 | Completed | Drug: AZD 8529 Drug: Risperidone |
Schizophrenia | AstraZeneca | June 2009 | Phase 2 |
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AZD8529 decreased nicotine priming-induced and cue-induced reinstatement in squirrel monkeys.Biol Psychiatry. 2015 Oct 1;78(7):452-62. |
Effect of AZD8529 on nicotine and food self-administration in squirrel monkeys.Biol Psychiatry. 2015 Oct 1;78(7):452-62. |
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