Comparative effect of l-CCG-I, DCG-IV and γ-carboxy-l-glutamate on all cloned metabotropic glutamate receptor subtypes

摘要: Abstract In a previous study we reported that the addition of carboxylic group to mGlu receptor agonist aminocyclopentane-1,3-dicarboxylate (ACPD) changes its properties from antagonist at both mGlu1 and mGlu2 receptors, resulted in an increase affinity mGlu4 with isomers being either agonists or antagonists. present study, effect γ-carboxy- l -glutamic acid (Gla) (2S,2′R,3′R)-2-(2,3-dicarboxycyclopropyl)glycine (DCG-IV), two derivatives non-selective agonists, were examined on all cloned receptors. We found this additional glutamate prevents interaction group-I receptors generates potent group-II (KB=55 μM mGlu2). At group-III Gla was be (mGlu7 mGlu8 receptors) partial (mGlu4 mGlu6 receptors). show here -CCG-I is general activating also confirm DCG-IV, which corresponds group, selective agonist. However, COOH making compound one most known so far. These observations will useful for development more