AZD 2066

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、高度 CNS 渗透性的 mGluR5 拮抗剂；抑制动物短暂的下食管括约肌松弛 (TLESR) 和胃酸反流。

A potent, selective, highly CNS-penetrant mGluR5 antagonist; inhibits transient lower oesophageal sphincter relaxations (TLESRs) in animals and acid reflux, shows potential for treatment of gastro-oesophageal reflux.Pain Phase 1 Discontinued.

AZD 2066 (1-10 μM) inhibits Ca2+ response, with IC50s of 27.2±9.1, 3.56±0.52, 96.2±17.8, and 380±78.0 nM in mGlu5/HEK cells and striatal, hippocampal, and cortical cultures respectively.AZD 2066 (1-10 μM) inhibits the oscillatory Ca2+ response which induced by bath application of DHPG, and blocks either DHPG or Quis e?ects in mGlu5/HEK cells.AZD 2066 (1-10 μM) has less e?ective in striatal neurons.

AZD 2066 (0.3-30 mg/kg; p.o.) shows discriminative effects in rats. Animal Model:Male Wistar rats (weighing 240-250 g) Dosage:0.03, 0.1, 0.3, 1, 3, 10, 30 mg/kg Administration:P.o. (60 minutes after administration)Result:Caused full and dose-dependent AZD9272-appropriate responding.

AZD-2066 | AZD2066

GPCR/G Protein

mGluR

mGluR

Neurological Disease

Pain

934282-55-0

381.82

C19H16ClN5O2

>98% (HPLC)

——

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

4-(5-{(1R)-1-[5-(3-chlorophenyl)isoxazol-3-yl]ethoxy}-4-methyl-4H-1,2,4-triazol-3-yl)pyridine

(-20℃)

With Ice Pack

≥ 2 years