AZD 2066 hydrate 

AZD-2066 hydrate is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydrate activates the BDNF/trkB signaling pathway. AZD 2066 hydrate can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease^[1][2][3][5].

AZD 2066 (1-10 μM) hydrate 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) hydrate 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.

AZD 2066 (0.3-30 mg/kg, p.o., 60 min) hydrate shows discriminative effects in rats^[2].
AZD-2066 (10 µM, perfusion of brain slide) hydrate 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) hydrate 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.

386.33

C₁₉H₁₆ClN₅O₂.1/4H₂O

Solid

Off-white to light yellow

CN1C(C2=CC=NC=C2)=NN=C1O[C@@H](C3=NOC(C4=CC(Cl)=CC=C4)=C3)C.O.[1/4]

Room temperature in continental US; may vary elsewhere.

• [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]