| Bioactivity | 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]. |
| Invitro | AZD 2066 (1-10 μM) hydrochloride 可抑制 Ca2+ 反应，在 mGlu5/HEK 细胞以及纹状体、海马和皮质培养物中的 IC50 分别为 27.2、3.56、96.2 和 380 nM[4]。AZD 2066 (1-10 μM) hydrochloride 可抑制 DHPG (HY-12598A) 浸浴诱导的 Ca2+ 振荡响应，并阻断 DHPG 或 Quis 在 mGlu5/HEK 细胞中的作用[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> AZD-2066 hydrochloride 相关抗体: |
| In Vivo | AZD 2066 (0.3-30 mg/kg，口服，60 min) hydrochloride 在大鼠中有辨别效应[2]。AZD-2066 (10 µM，脑切片灌注) hydrochloride 通过 BDNF/trkB 信号通路减轻慢性社会挫败应激 (CSDS) 处理小鼠中 dihydroxyphenylglycine (DHPG) 促进的长期抑郁 (LTD)[5]。AZD-2066 (5 mg/kg，腹腔注射，2 × 12 h) hydrochloride 可减轻小鼠中慢性社会挫败应激 (CSDS) 诱发的抑郁行为[5]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 934338-70-2 |
| Formula | C19H17Cl2N5O2 |
| Molar Mass | 418.28 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. [3]. Antoniu SA. Discontinued drugs for pulmonary, allergy, gastrointestinal, arthritis (2012). Expert Opin Investig Drugs. 2013 Nov;22(11):1453-64. [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. [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. |
AZD-2066 hydrochloride
CAS: 934338-70-2 F: C19H17Cl2N5O2 W: 418.28
AZD-2066 hydrochloride is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydr
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