AZD-2066 hydrochloride
Based on 1 publication(s) in Google Scholar
AZD-2066 hydrochloride is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydrochloride activates the BDNF/trkB signaling pathway. AZD 2066 hydrochloride can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease.
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- CAS. Nr.: 934338-70-2
- Formel: C19H17Cl2N5O2
- Molecular Weight:418.28
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Other In-stock Forms of AZD-2066 hydrochloride
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) AZD-2066 hydrochloride
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Biologische Aktivität
Beschreibung
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mGluR5 |
In Vitro
AZD 2066 (1-10 μM) hydrochloride inhibits Ca2+ response, with IC50s of 27.2, 3.56, 96.2, and 380 nM in mGlu5/HEK cells and striatal, hippocampal, and cortical cultures respectively[4].
AZD 2066 (1-10 μM) hydrochloride inhibits the oscillatory Ca2+ response which induced by bath application of DHPG (HY-12598A), and blocks either DHPG or Quis effects in mGlu5/HEK cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AZD-2066 (10 µM, perfusion of brain slide) hydrochloride alleviates dihydroxyphenylglycine (DHPG)-facilitated long-term depression (LTD) expression in chronic social defeat stress (CSDS)-treated mice via BDNF/trkB signaling pathway[5].
AZD-2066 (5 mg/kg, i.p., 2 × 12 h) hydrochloride alleviates chronic social defeat stress (CSDS)-induced depressive behaviors in mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (weighing 240-250 g)[2]
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Dosage:0.03, 0.1, 0.3, 1, 3, 10, 30 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Caused full and dose-dependent AZD9272-appropriate responding.
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Animal Model:Depressive model (C57BL/6 mice were subjected to physical defeats that were generated by a CD-1 aggressor for 5 min every day for 10 days)[5]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection (i.p.), 2 × 12 h
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Result:Increased social interaction ratio.
Reversed time spent in interaction zone.
Increased sucrose preference scores.
Chemical Information
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CAS. Nr. 934338-70-2
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Molecular Weight 418.28
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Formel C19H17Cl2N5O2
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SMILES
CN1C(C2=CC=NC=C2)=NN=C1O[C@@H](C3=NOC(C4=CC(Cl)=CC=C4)=C3)C.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Chem Neurosci
Location and Cell-Type-Specific Bias of Metabotropic Glutamate Receptor, mGlu5, Negative Allosteric Modulators. [Abstract]2019 Nov 20;10(11):4558-4570. PMID: 31609579
Reinheit & Dokumentation
Verweise
[1]. Kågedal M, et al. A positron emission tomography study in healthy volunteers to estimate mGluR5 receptor occupancy of AZD2066-estimating occupancy in the absence of a reference region. Neuroimage. 2013 Nov 15;82:160-9. [Content Brief]
[2]. Swedberg MD, et al. AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects. J Pharmacol Exp Ther. 2014 Aug;350(2):212-22. [Content Brief]
[3]. Antoniu SA. Discontinued drugs for pulmonary, allergy, gastrointestinal, arthritis (2012). Expert Opin Investig Drugs. 2013 Nov;22(11):1453-64. [Content Brief]
[4]. Jong YI, et al. Location and Cell-Type-Specific Bias of Metabotropic Glutamate Receptor, mGlu5, Negative Allosteric Modulators. ACS Chem Neurosci. 2019 Nov 20;10(11):4558-4570. [Content Brief]
[5]. Jiang X, et al. mGluR5 Facilitates Long-Term Synaptic Depression in a Stress-Induced Depressive Mouse Model. Can J Psychiatry. 2020 May;65(5):347-355. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AZD-2066 hydrochloride Related Classifications
HY-110255B Related Classifications
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