生物活性 | |||
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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 | |||
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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 |
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