AZD-2066 hydrochloride

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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.

For research use only. We do not sell to patients.

AZD-2066 hydrochloride Chemical Structure

CAS No. : 934338-70-2

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Other Forms of AZD-2066 hydrochloride:

AZD 2066 Get quote

1 Publications Citing Use of MCE AZD-2066 hydrochloride

•ACS Chem Neurosci. 2019 Nov 20;10(11):4558-4570. [Abstract]

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•Related Small Molecules:

•Related Proteins:

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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TrkA TrkB TrkC Trk

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]^[3]^[5]

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 (0.3-30 mg/kg, p.o., 60 min) hydrochloride shows discriminative effects in rats^[2].
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.

Animal Model:	Male Wistar rats (weighing 240-250 g)^[2]
Dosage:	0.03, 0.1, 0.3, 1, 3, 10, 30 mg/kg
Administration:	Oral gavage (p.o.)
Result:	Caused full and dose-dependent AZD9272-appropriate responding.

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]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection (i.p.), 2 × 12 h
Result:	Increased social interaction ratio. Reversed time spent in interaction zone. Increased sucrose preference scores.

Molecular Weight

418.28

Formula

C₁₉H₁₇Cl₂N₅O₂

CAS No.

934338-70-2

SMILES

CN1C(C2=CC=NC=C2)=NN=C1O[C@@H](C3=NOC(C4=CC(Cl)=CC=C4)=C3)C.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]