• NMDA receptor
  • AMPA receptor
  • mGluR2
  • mGluR3
  • mGluR4
  • mGluR5

mGluR5 选择性激动剂 | 拮抗剂 | 调节剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S2861 CTEP (RO4956371) CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors. Selective mGlu5, IC50: 2.2 nM
S1970 VU-29 VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor, with EC50 of 9 nM and Ki=244 nM for rat mGluR5, which is selective for mGluR5 relative to other mGluR subtypes. Selective rat mGluR5, EC50: 9 nM; rat mGluR5, Ki: 244 nM
S2795 VU 0357121 VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes. Selective mGluR5, EC50: 30 nM
S2809 MPEP MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors. Selective mGluR5, IC50: 36 nM
S2690 ADX-47273 ADX47273 (BA 94673139) is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes. Selective mGlu5, EC50: 0.17 μM
S2645 SIB 1757 SIB 1757 is a highly selective, noncompetitive antagonist of metabotropic glutamate receptor type 5 (mGluR5) with IC50 of 0.4 μM at hmGluR5 compared with >30 µM at hmGluR1b, hmGluR2, hmGluR4, hmGluR6, hmGluR7 and hmGluR8. Selective mGluR5, IC50: 0.4 μM
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