CPPG
関連概念 : 化学

[(RS)-a-Cyclopropyl-4-phosphonophenylglycine]

C11H14NO5P(271.21)。

   

Potent group II/III mGluR(mGluR6)のアンタゴニスト。
group IIIに選択的に働き(IC50=2.2nM)、group II(IC50=46.2nM)に対する選択性は20倍。
neonatal rat cortical slicesではより弱いgroup I mGluRのアンタゴニスト(Kb = 0.65 ± 0.07 nM)。

【性質】

  ・Soluble to 100 mM in 1eq. NaOH
  ・Store at RT

【参考】

   Kemp et al (1996) α-Methyl-3-phosphonophenylglycine and α-cyclopropyl-4-phosphonophenylglycine are potent antagonists at mGluRs negatively coupled to adenylyl cyclase. Br.J.Pharmacol. (Abstr) 117 (in press).
   Toms et al (1996) The effects of (RS)-α-cyclopropyl-4-phosphonophenylglycine ((RS)-CPPG), a potent and selective metabotropic glutamate receptor antagonist. BrJ.Pharmacol. 119 851.
   Jane et al (1996) Potent antagonists at the L-AP4- and (1S3S)-ACPD-sensitive presynaptic metabotropic glutamate receptors in the neonatal rat spinal cord. Neuropharmacology 35 1029
   Nawy,2004タイガーサラマンダーmGluR6脱感作

2010/03/22 masashi tanaka

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