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GABAA receptor
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=== Types === [[File:6X3Z GABAAR GABA.png|thumb|GABA bound at its orthosteric site in the beta-alpha interface of an α1β2γ2 GABAA receptor. H-atoms hidden.]] * [[Agonist|Orthosteric agonists]] and [[Receptor antagonist|antagonists]]<!--inverse agonists?-->: bind to the main receptor site (the site where GABA normally binds, also referred to as the "active" or "orthosteric" site). Agonists activate the receptor, resulting in increased {{chem|Cl|-}} conductance. Antagonists, though they have no effect on their own, compete with GABA for binding and thereby inhibit its action, resulting in decreased {{chem|Cl|-}} conductance. * [[Allosteric modulator|First order allosteric modulators]]: bind to allosteric sites on the receptor complex and affect it either in a positive (PAM), negative (NAM) or neutral/silent (SAM) manner, causing increased or decreased efficiency of the main site and therefore an indirect increase or decrease in {{chem|Cl|-}} conductance. SAMs do not affect the conductance, but occupy the binding site. * [[Allosteric modulator|Second order modulators]]: bind to an allosteric site on the receptor complex and modulate the effect of first order modulators. * [[Channel blocker|Open channel blockers]]: prolong ligand-receptor occupancy, activation kinetics and Cl ion flux in a subunit configuration-dependent and sensitization-state dependent manner.<ref>{{cite journal | vauthors = Haseneder R, Rammes G, Zieglgänsberger W, Kochs E, Hapfelmeier G | title = GABA(A) receptor activation and open-channel block by volatile anaesthetics: a new principle of receptor modulation? | journal = European Journal of Pharmacology | volume = 451 | issue = 1 | pages = 43–50 | date = September 2002 | pmid = 12223227 | doi = 10.1016/S0014-2999(02)02194-5 }}</ref> * [[Channel blocker|Non-competitive channel blockers]]: bind to or near the central pore of the receptor complex and directly block {{chem|Cl|-}} conductance through the ion channel.
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