您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > ZJ 43
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
ZJ 43
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ZJ 43图片
CAS NO:723331-20-2
包装:10mg
规格:98%
市场价:4683元
分子量:304.3

产品介绍
GCP II and III/NAAG peptidase/NAALADase inhibitor
CAS:723331-20-2
分子式:C12H20N2O7
分子量:304.3
纯度:98%
存储:Store at -20°C

Background:

IC50: 2.4 nM


ZJ-43 is a N-acetylaspartylglutamate (NAAG) peptidase inhibitor.


The peptide neurotransmitter N-acetylaspartylglutamate (NAAG) is reported to act as an agonist at group II metabotropic glutamate receptors. NAAG is inactivated by extracellular peptidase activity leading to yielding glutamate and N-acetylaspartate.


In vitro: As a potent inhibitor of glutamate carboxypeptidase II and III (GCP II and III) with Kivalues of 0.8 and 23 nM respectively, ZJ-43 inhibited the hydrolysis of NAAG via indirect interactions with NMDA or metabotropic glutamate receptors [1].


In vivo: Intravenous injection of ZJ-43 coiuld suppress both phases of the agitation behaviour induced by paw formalin injection in the rat neuropathic pain model. Moreover, intravenous administration of ZJ-43 attenuated the level of mechanical allodynia induced by the nerve ligation. These effects of ZJ-43 in both the formalin test and the partial sciatic nerve ligation model were completely antagonized by pretreatment with LY-341495, which was a highly selective group II mGluR antagonist [1].


Clinical trial: N/A


Reference:
[1] Yamamoto T1,Hirasawa S,Wroblewska B,Grajkowska E,Zhou J,Kozikowski A,Wroblewski J,Neale JH.  Antinociceptive effects of N-acetylaspartylglutamate (NAAG) peptidase inhibitors ZJ-11, ZJ-17 and ZJ-43 in the rat formalin test and in the rat neuropathic pain model. Eur J Neurosci.2004 Jul;20(2):483-94.