PHAR 562 Lecture Notes - Lecture 4: Electrophysiology, Peptide, Conformational Change
14 Oct 2017
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2 functional ampar families containing glua2 and lacking. Subject to alternate splicing and rna editing. Qr site of glua2 is the only ampar subunit that is edited. Glua2 containing = ca impermeable, polyamine insensitive, low unitary conductance. Glua2 lacking = ca permeable, polyamine sensitive, high unitary conductance. Several mechanisms are designed to relieve ampar polyamine block. Ampars assemble in complex with aux proteins which affect trafficking and gating. Nmdars act as coincidence detectors: relies on mg block. Activation has an absolute requirement for glutamate and glycine: both needed in order to activate these receptors. Each nt binds to different family of receptor subunits: gly to glun1, glu to glun2a-d. Expression profile of glun1 overlaps with glun2a-d. Different glun2 subunits impart distinct functional properties. Nmdars are regulated by a number of endogenous modulators. Koff or off-rate is the time it stays bound to whatever it is binding. Affinity (kd) = koff/kon (the smaller the kd, the higher the affinity)
