PHIL 2015 Chapter Notes - Chapter 3.4: Carbonic Anhydrase Inhibitor, Histone Deacetylase Inhibitor, Aromatase Inhibitor
23 May 2020
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Nicotinic acetylcholine receptors/ acetylcholinesterase: varenicline: partial agonist at 4 7 nachr and full agonist at 7 channels. Indication: smoking cessation therapy: mecamylamine: noncompetitive open channel blocker of nachrs. Gabaa receptors: acetazolamide: carbonic anhydrase inhibitor ( [hco3. Indication: chronic pain, hyperalgesia: clp257: increases surface expression of kcc2 ( [cl-]intracellular and eo. Indication: treatment of neuropathic nerve injury: anesthetics (e. g. , sevoflurane, etomidate): binds at the interface of certain gabaa subunits. Etomidate binds to the 5- subunit (highly expressed in the hippocampus) Indication: numbs pain for surgical intervention: benzodiazepines: binds at the interface of - and -subunits of gabaa (no sites on -subunits) using several important key residues including histidine-101. Results in an increase in single channel mean open time overall gaba potency (i. e. , Glutamate receptors: cyclothiazide: inhibits desensitization of ampar channel remains open in the presence of agonist: ketamine: binds to the open pore of nmdar similar to mg2+ blockade without subunit specificity.
