Agonists: Difference between revisions

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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]].

'''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]].

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@@ Line 18: / Line 18: @@
 '''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]].