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 > Lu AF21934
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:
 
Lu AF21934
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。
Lu AF21934图片
CAS NO:1445605-23-1
规格:98%
分子量:315.2
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
positive allosteric modulator of mGlu4 receptors
CAS:1445605-23-1
分子式:C14H16Cl2N2O2
分子量:315.2
纯度:98%
存储:Store at -20°C

Background:

EC50: 500 nM


Lu AF21934 is a positive allosteric modulator of mGlu4 receptors.


The mGlu4 receptor subtype of the group III mGlu is mainly a presynaptic auto- or hetero-receptor. Its stimulation results in an inhibition of glutamatergic or GABAergic transmission and release


In vitro: Lu AF21934 has been identified as a brain-penetrating positive allosteric modulator of mGlu4 receptors. In broad in-vitro screens, Lu AF21934 could potentiate the glutamate response at the mGlu4 receptor with an Emax=120% and a glutamate fold-shift FS=5. Lu AF21934 did not showed any significant affinity for 70 GPCRs at 10 μM, but acted as a weak positive allosteric modulator of mGlu6 receptor, as well as an antagonist of adenosine A2A and 5-HT2B receptors [1].


In vivo: In rats, harmaline triggered tremor as manifested by an increase in the power within 9-15Hz band and in the tremor index. Harmaline also induced a biphasic effect on mobility, initially inhibiting the exploratory locomotor activity of rats, followed by an increase in their basic activity. Lu AF21934 at 0.5-5 mg/kg sc did not influence tremor but at doses of 0.5 and 2.5 mg/kg reversed harmaline-induced hyperactivity. MGlu4 mRNA expression was found to be high in the cerebellar cortex and low in the inferior olive [1].


Clinical trial: Up to now, Lu AF21934 is still in the preclinical development stage.


Reference:
[1] Ossowska K,Wardas J,Berghauzen-Maciejewska K,et al.  Lu AF21934, a positive allosteric modulator of mGlu4 receptors, reduces the harmaline-induced hyperactivity but not tremor in rats. Neuropharmacology.2014 Aug;83:28-35.