ADMS 3502 Lecture 27: Alpha 1 GABAA
21 May 2020
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Related to bz in function binds to bz site of gabaa increases channel open time. Much shorter half life than typical benzodiazepines: lorazepam (benzo): 12-18 hrs, zolpidem (non-benzo): 2. 5-4 hrs. Slide 79: glun2 subunits determine many properties of the nmda receptor. Glun2a and glun2b receptor have the lowest agonist potency, but they have the fastest deactivation rate. The glun2a and glun2b have the higher mg2+ sensitivity, and ca2+ permeability-they have the highest conductance overall. Are normally blocked by mg2+ ionslike a cork, but blockade is relieved by depolarization as mg2+ is expelled from the pore. Memantine is a nmda antagonist that can block extrasynaptic nmda. It can promote cell survival and prevent excitotoxicity and death in stroke. Very short window for therapeutic intervention because traumatic brain injury and stroke leads to increased ec glutamate and hence severe excitotoxicity. Dysregulation of ec ionic composition exacerbates nmda toxicity.
