AZD8529 mesylate

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

AZD8529 是一种新型有效、选择性 mGluR2 正变构调节剂，EC50 为 195 nM。

AZD8529 is a novel potent, selective mGluR2 positive allosteric modulator with EC50 of 195 nM, does not produce any positive allosteric modulator responses for mGluR1 and 3-8 subtypes; potentiates agonist-induced activation of mGluR2 in the membrane-binding assay and in primate cortex, hippocampus and striatum; decreases nicotine self-administration at doses (0.3-3 mg/kg) in monkeys, also reduces nicotine priming- and cue-induced reinstatement of nicotine seeking, decreases nicotine-induced accumbens dopamine release in rats.Schizophrenia Phase 2 Discontinued(In Vitro):AZD-8529 mesylate potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM .AZD-8529 mesylate does not elicit antagonist responses on mGluRs at 25 μM.(In Vivo):AZD-8529 mesylate (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys.AZD-8529 mesylate (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats.

AZD-8529 mesylate potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM .AZD-8529 mesylate does not elicit antagonist responses on mGluRs at 25 μM.

AZD-8529 mesylate (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys. AZD-8529 mesylate (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats. Animal Model:Sprague-Dawley rats Dosage:10 mg/kg, 30 mg/kg Administration:Intraperitoneal injection; 2 hours before nicotine injections Result:Decreased the increased extracellular dopamine induced by nicotine (0.4 mg/kg, s.c.) in accumbens shell of freely-moving rats.

AZD 8529 mesylate

GPCR/G Protein

mGluR

mGluR

Neurological Disease

Schizophrenia

1314217-69-0

583.583

C25H28F3N5O6S

>98% (HPLC)

In Vitro:?DMSO : 41.67 mg/mL (71.40 mM)

CC1=CC(=CC2=C1C(=O)N(C2)CC3=CC=C(C=C3)OC(F)(F)F)C4=NC(=NO4)CN5CCNCC5.CS(=O)(=O)O

7-methyl-5-(3-(piperazin-1-ylmethyl)-1,2,4-oxadiazol-5-yl)-2-(4-(trifluoromethoxy)benzyl)isoindolin-1-one methanesulfonate

(-20℃)

With Ice Pack

≥ 2 years