"目录号: HY-13694
Membrane Transporter/Ion ChannelNeuronal Signaling-
MRX-1024 是一种有效的化学保护剂，它还可以通过激活GABAA受体来抑制神经元活性。
GABA Receptor
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生物活性
Description
MRX-1024 is an effective chemoprotective agent which can also inhibit the neuronal activity throughGABAAreceptor activation.
IC50& Target
GABAAreceptor[1]
In Vitro
The incubation of human plasma with MRX-1024 (D-methionine) and CP leads to the formation of a Pt-D-methionine complex independent of the order of addition. In plasma, an early CP hydrolysis product reacts with MRX-1024 to form a 1:1 complex that is followed by the formation of a 2:1 compound at a later time point. The formation of these Pt-D-methionine species plays an important role in the processes by which MRX-1024 protects mammalian organisms against CP-induced toxicities[2].
In Vivo
When MRX-1024 (D-methionine) is administered along with cisplatin the cell density is 0.8±0.070 (SEM), significantly larger than in rats treated with only cisplatin (P<0.01) while not significantly different from controls or from animals treated only with D-methionine (P>0.05). When MRX-1024 is administered alone the average cell density is 0.95±0.099 (SEM) and not significantly different from controls (P>0.05)[3].
References
[1].Wu C, et al. Antioxidants L-carnitine and D-methionine modulate neuronal activity through GABAergic inhibition. J Neural Transm (Vienna). 2014 Jul;121(7):683-93.
[2].Sooriyaarachchi M, et al. Chemoprotection by D-methionine against cisplatin-induced side-effects: insight from in vitrostudies using human plasma. Metallomics. 2014 Mar;6(3):532-41.
[3].Hinduja S, et al. D-methionine protects against cisplatin-induced neurotoxicity in the hippocampus of the adult rat. Neurotox Res. 2015 Apr;27(3):199-204.