Search results
Results from the WOW.Com Content Network
Examples of ligands activating peroxisome proliferator-activated receptor gamma as partial agonists are honokiol and falcarindiol. [3] [4] Delta 9-tetrahydrocannabivarin is a partial agonist at CB2 receptors and this activity might be implicated in ∆9-THCV-mediated anti-inflammatory effects. [5]
An example is the cannabinoid inverse agonist rimonabant. A superagonist is a term used by some to identify a compound that is capable of producing a greater response than the endogenous agonist for the target receptor. It might be argued that the endogenous agonist is simply a partial agonist in that tissue.
Lorcaserin is a full agonist for 5-HT 2C and 5-HT 2B receptors and partial agonist for 5-HT 2A receptors (75% of the maximal response elicited by serotonin). [7] Lorcaserin is a potent and selective 5-HT 2C agonist with rapid oral absorption that shows dose-dependent decrease in food intake and body weight.
Methysergide – a congener of methylergonovine, used in treatment of migraine blocks 5-HT 2A and 5-HT 2C receptors, but sometimes acts as partial agonist, in some preparations. Piperidine derivatives such as OSU-6162, which acts as a partial agonist at both 5-HT 2A and dopamine D 2 receptors, and Z3517967757.
A nicotinic agonist is a drug that mimics the action of acetylcholine (ACh) at nicotinic acetylcholine receptors (nAChRs). The nAChR is named for its affinity for nicotine. Examples include nicotine (by definition), acetylcholine (the endogenous agonist of nAChRs), choline, epibatidine, lobeline, varenicline and cytisine. [1]
In addition, depending on the cell type, the specific effect, whether agonist, antagonist, inverse agonist, etc., could have a unique specific effect. An example is seen in insulin, under "Receptor Agonists," as it interacts with multiple different cell types as an agonist, but incites multiple and different responses in both.
Gepirone (partial agonist, K i = 70 nM) Haloperidol; Ipsapirone (partial agonist, K i = 12.1 nM) Quetiapine; Trazodone (SARI, selective in the sense that on all other 5-HT receptors it acts as either an antagonist or has no action. K d = 78 nM) Yohimbine (unselective partial agonist) Tandospirone (potent and selective partial agonist) Nonselective
PAM-agonists work like PAMs, but also as agonists with and without the agonists they modulate. [4] PAM-antagonists work like PAMs, but also function as antagonists and lower the efficacy of the agonists they modulate. [4] negative allosteric modulators (NAM) lower agonist affinity and/or efficacy. [4] Maraviroc is a medicine that modulates CCR5.