AZD-8529 mesylate
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MedKoo CAT#: 529803

CAS#: 1314217-69-0 (mesylate)

Description: AZD-8529 is a a positive allosteric modulator at the mGluR2 receptor. AZD8529 decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. AZD8529 potentiated agonist-induced activation of mGluR2 in the membrane-binding assay and in primate cortex, hippocampus, and striatum. In monkeys, AZD8529 decreased nicotine self-administration at doses (.3-3 mg/kg) that did not affect food self-administration. AZD8529 also reduced nicotine priming- and cue-induced reinstatement of nicotine seeking after extinction of the drug-reinforced responding. In rats, AZD8529 decreased nicotine-induced accumbens dopamine release. The positive allosteric modulators of metabotropic glutamate receptor 2 should be considered for relapse prevention.

Chemical Structure

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AZD-8529 mesylate
CAS# 1314217-69-0 (mesylate)
Instruction

Theoretical Analysis

MedKoo Cat#: 529803
Name: AZD-8529 mesylate
CAS#: 1314217-69-0 (mesylate)
Chemical Formula: C25H28F3N5O6S
Exact Mass: 487.18
Molecular Weight: 583.583
Elemental Analysis: C, 51.45; H, 4.84; F, 9.77; N, 12.00; O, 16.45; S, 5.49

Price and Availability

Size Price Availability Quantity
50mg USD 1250 2 Weeks
100mg USD 1950 2 Weeks
200mg USD 2950 2 Weeks
500mg USD 4650 2 Weeks
1g USD 6450 2 Weeks
2g USD 8950 2 Weeks
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Related CAS #: 1092453-15-0 (free base)   1314217-69-0 (mesylate)   1344999-56-9 (mesylate hydrate)    

Synonym: AZD-8529; AZD8529; AZD 8529; AZD-8529 mesylate

IUPAC/Chemical Name: 7-methyl-5-(3-(piperazin-1-ylmethyl)-1,2,4-oxadiazol-5-yl)-2-(4-(trifluoromethoxy)benzyl)isoindolin-1-one mesylate

InChi Key: HRHCPVNKPOTCGB-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H24F3N5O3.CH4O3S/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;1-5(2,3)4/h2-5,10-11,28H,6-9,12-14H2,1H3;1H3,(H,2,3,4)

SMILES Code: O=C1N(CC2=CC=C(OC(F)(F)F)C=C2)CC3=C1C(C)=CC(C4=NC(CN5CCNCC5)=NO4)=C3.OS(=O)(C)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 583.58 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Justinova Z, Panlilio LV, Secci ME, Redhi GH, Schindler CW, Cross AJ, Mrzljak L, Medd A, Shaham Y, Goldberg SR. The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. Biol Psychiatry. 2015 Oct 1;78(7):452-62. doi: 10.1016/j.biopsych.2015.01.014. PubMed PMID: 25802079; PubMed Central PMCID: PMC4529372.

2: Augier E, Dulman RS, Rauffenbart C, Augier G, Cross AJ, Heilig M. The mGluR2 Positive Allosteric Modulator, AZD8529, and Cue-Induced Relapse to Alcohol Seeking in Rats. Neuropsychopharmacology. 2016 Nov;41(12):2932-2940. doi: 10.1038/npp.2016.107. PubMed PMID: 27339394; PubMed Central PMCID: PMC5061885.

3: Litman RE, Smith MA, Doherty JJ, Cross A, Raines S, Gertsik L, Zukin SR. AZD8529, a positive allosteric modulator at the mGluR2 receptor, does not improve symptoms in schizophrenia: A proof of principle study. Schizophr Res. 2016 Apr;172(1-3):152-7. doi: 10.1016/j.schres.2016.02.001. PubMed PMID: 26922656.

4: Caprioli D, Venniro M, Zeric T, Li X, Adhikary S, Madangopal R, Marchant NJ, Lucantonio F, Schoenbaum G, Bossert JM, Shaham Y. Effect of the Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor 2 AZD8529 on Incubation of Methamphetamine Craving After Prolonged Voluntary Abstinence in a Rat Model. Biol Psychiatry. 2015 Oct 1;78(7):463-73. doi: 10.1016/j.biopsych.2015.02.018. PubMed PMID: 25861699; PubMed Central PMCID: PMC4546920.

5: Li X, D'Souza MS, Niño AM, Doherty J, Cross A, Markou A. Attenuation of nicotine-taking and nicotine-seeking behavior by the mGlu2 receptor positive allosteric modulators AZD8418 and AZD8529 in rats. Psychopharmacology (Berl). 2016 May;233(10):1801-14. doi: 10.1007/s00213-016-4220-2. PubMed PMID: 26873083.

6: Acri JB, Cross AJ, Skolnick P. From bench to bedside: mGluR2 positive allosteric modulators as medications to treat substance use disorders. Psychopharmacology (Berl). 2016 Dec 20. [Epub ahead of print] Review. PubMed PMID: 27995279.