Agonists: Difference between revisions
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<StructureSection load='' size='350' side='right' scene=' | <StructureSection load='2ace' size='350' side='right' scene='2ace/Com_view/1' caption='Torpedo californica acetylcholinesterase complex with acetylcholine, [[2ace]]' > | ||
'''Agonists'''. A ligand that can bind to and alter the function of the receptor that triggers a physiological response is called a receptor '''agonist'''. | '''Agonists'''. A ligand that can bind to and alter the function of the receptor that triggers a physiological response is called a receptor '''agonist'''. | ||
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'''Selective agonist''' is selective for a specific type of receptor. E.g. buspirone is a selective agonist for serotonin 5-HT1A (see [[5-hydroxytryptamine receptor]]. | '''Selective agonist''' is selective for a specific type of receptor. E.g. buspirone is a selective agonist for serotonin 5-HT1A (see [[5-hydroxytryptamine receptor]]. | ||
'''Partial agonists''' (such as buspirone, aripiprazole, buprenorphine, or norclozapine) also bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist, even at maximal receptor occupancy. Agents like buprenorphine are used to treat opiate dependence for this reason, as they produce milder effects on the opioid receptor (see [[μ Opioid Receptors]]) with lower dependence and abuse potential. Examples of ligands activating [[PPAR-gamma|peroxisome proliferator-activated receptor gamma]] as partial agonists are honokiol and falcarindiol. | '''Partial agonists''' (such as buspirone, [[aripiprazole]], buprenorphine, or norclozapine) also bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist, even at maximal receptor occupancy. Agents like buprenorphine are used to treat opiate dependence for this reason, as they produce milder effects on the opioid receptor (see [[μ Opioid Receptors]]) with lower dependence and abuse potential. Examples of ligands activating [[PPAR-gamma|peroxisome proliferator-activated receptor gamma]] as partial agonists are honokiol and falcarindiol. | ||
'''Inverse agonist''' is an agent that binds to the same receptor binding-site as an agonist for that receptor and inhibits the constitutive activity of the receptor. The opioid antagonists naloxone and naltrexone are also partial inverse agonists at [[μ Opioid Receptors]]. Nearly all antihistamines acting at [[Histamine H1 receptor|H1 receptors]] and H2 receptors have been shown to be inverse agonists. The beta blockers carvedilol and bucindolol have been shown to be low level inverse agonists at [[Beta-2 adrenergic receptor|beta adrenoreceptors]]. | '''Inverse agonist''' is an agent that binds to the same receptor binding-site as an agonist for that receptor and inhibits the constitutive activity of the receptor. The opioid antagonists naloxone and naltrexone are also partial inverse agonists at [[μ Opioid Receptors]]. Nearly all antihistamines acting at [[Histamine H1 receptor|H1 receptors]] and H2 receptors have been shown to be inverse agonists. The beta blockers carvedilol and bucindolol have been shown to be low level inverse agonists at [[Beta-2 adrenergic receptor|beta adrenoreceptors]]. | ||