(S)-4CPG

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Chemical Structure| 134052-73-6 同义名 : (S)-4-Carboxyphenylglycine
CAS号 : 134052-73-6
货号 : A462285
分子式 : C9H9NO4
纯度 : 97%
分子量 : 195.17
MDL号 : MFCD00216831
存储条件:

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 (S) -4CPG acts as competitive antagonists for mGluR1 with pA2 values of 4.46[1]. Early (S)-4CPG treatment significantly attenuated the development of mechanical allodynia (90 and 270 nmol) and cold hyperalgesia (270 nmol). However, late treatment with (S)-4CPG did not reduce the nociceptive behaviours in either behavioural task[2]. The decrease in the seizure threshold for pentylenetetrazole during diazepam withdrawal was significantly suppressed by intracerebroventricular (i.c.v.) pretreatment with the group 1 mGlu receptor antagonist, (S)-4-carboxyphenylglycine ((S)-4CPG: 56 and 100 nmol)[3]. i.t. treatment with MK-801 significantly reduced nociceptive scores in the formalin test and also produced a significant suppression of formalin-induced increases in [3H]-PDBu binding in laminae I-II, III-VI and X of the lumbar spinal cord. In contrast, i.t. treatment with (S)-4CPG failed to significantly affect either nociceptive behaviours in the formalin test or formalin-induced increases in [3H]-PDBu binding in laminae I-II and III-VI of the lumbar spinal cord. On the other hand, i.t. treatment with either MK-801 or (S)-4CPG produced a significant reduction in mechanical and cold hypersensitivity, as well as [3H]-PDBu binding in laminae I-II and III-VI of the lumbar spinal cord, after CCI(chronic constriction injury)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.12mL

1.02mL

0.51mL

25.62mL

5.12mL

2.56mL

51.24mL

10.25mL

5.12mL

参考文献

[1]Hayashi Y, Sekiyama N, Nakanishi S, Jane DE, Sunter DC, Birse EF, Udvarhelyi PM, Watkins JC. Analysis of agonist and antagonist activities of phenylglycine derivatives for different cloned metabotropic glutamate receptor subtypes. J Neurosci. 1994 May;14(5 Pt 2):3370-7

[2]Fisher K, Fundytus ME, Cahill CM, Coderre TJ. Intrathecal administration of the mGluR compound, (S)-4CPG, attenuates hyperalgesia and allodynia associated with sciatic nerve constriction injury in rats. Pain. 1998 Jul;77(1):59-66

[3]Suzuki T, Shimizu N, Tsuda M, Soma M, Misawa M. Role of metabotropic glutamate receptors in the hypersusceptibility to pentylenetetrazole-induced seizure during diazepam withdrawal. Eur J Pharmacol. 1999 Mar 19;369(2):163-8

[4]Yashpal K, Fisher K, Chabot JG, Coderre TJ. Differential effects of NMDA and group I mGluR antagonists on both nociception and spinal cord protein kinase C translocation in the formalin test and a model of neuropathic pain in rats. Pain. 2001 Oct;94(1):17-29