GLUTAMATE RECEPTORS Flashcards
this receptor includes ligand binding sites and ion channels (no g-protein are involved)
NMDA receptors
the primary ligand binding site of the NMDA receptor is what? what inhibits this?
glutamate or exogenous NMDA (N-methyl-D-aspartate)
AP-5
what makes the NMDA receptor unique? (hint 2 other agonist sites)
the requirement for the binding of 2 other agonists simultaneously with glutamate to activate the channel
glutamate site (+glutamate -AP-5) glycine site (+glycine -kynurenic acid) polyamine site (+spermidine -diethylenetriamine, enhances)
the ion channel of the NMDA is decreased by?
high Mg++, MK-801, ketamine (special K), phencyclidine (PCP or angel dust)
this receptor is also called a quisqualate receptor and is widely distributed throughout the CNS. This is a single protein complex containing a Na/Ca pore?
ampa receptor
agonist and antagonist of the ampa receptors?
agonist: glutamate, ampa
antagonist: NBQX
this receptor is a toxin from algae, and it is an agonist at these receptors? no antagonist for this?
kainate receptor
agonist: glutamate and kainate
these were the most recently discovered class of glutamate receptors and have two subtypes, both using g proteins to link effectors?
metabotropic receptors
AP-4
ACPD
this metabotropic receptor activates phosphodiesterase in target cells, which catabolizes cAMP and cGMP. AP-4 activation decreases glutamate release suggesting that at least some of these receptors function in presynaptic inhibition of glutamatergic terminals?
AP-4 receptors
this metabotropic receptor activation results in phospholipase C stimulation (increase DAG and IP3 leading to CA+) Like AP-4 receptors, ACPD appears to modulate the impact of other synapses?
ACPD receptors
the Ca++conductance of NMDA channels has been implicated in stimulating _____? what else has it been implicated in?
plasticity
post ischemic cell damage/death, this model called excitotoxicity, the NMDA antagonist MK-801 decreasing excitotoxicity
these diseases also involve NMDA and AMPA receptor activation?
ALS (lou Gehrigs disease) and Huntington’s disease