| Hazard Information | Back Directory | [Uses]
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[1][2][3][5]. | [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].
| 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.
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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] | | 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.
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| [IC 50]
mGluR5 | [References]
[1] K?gedal 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. DOI:10.1016/j.neuroimage.2013.05.006
[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. DOI:10.1124/jpet.114.215137
[3] Antoniu SA. Discontinued drugs for pulmonary, allergy, gastrointestinal, arthritis (2012). Expert Opin Investig Drugs. 2013 Nov;22(11):1453-64. DOI:10.1517/13543784.2013.836489
[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. DOI:10.1021/acschemneuro.9b00415
[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. DOI:10.1177/0706743719874162 |
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