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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.
This is a list of miscellaneous agonists of the serotonin receptor subtype 5-HT 2A (and other 5-HT 2 subtypes to a varying extent) ...
5-HT receptors were split into two classes by John Gaddum and Picarelli when it was discovered that some of the serotonin-induced changes in the gut could be blocked by morphine, while the remainder of the response was inhibited by dibenzyline, leading to the naming of M and D receptors, respectively. 5-HT 2A is thought to correspond to what was originally described as D subtype of 5-HT ...
5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems. [ 1 ] [ 2 ] [ 3 ] They mediate both excitatory and inhibitory neurotransmission .
A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin (5-hydroxytryptamine; 5-HT), a neurotransmitter and hormone and the endogenous ligand of the serotonin receptors.
These effects are the result of activation of 5-HT 1A receptors within the rostral ventrolateral medulla. [10] The sympatholytic antihypertensive drug urapidil is an α 1-adrenergic receptor antagonist and 5-HT 1A receptor agonist, and it has been demonstrated that the latter property contributes to its overall therapeutic effects.
Some drugs that act as 5-HT 4 agonists are also active as 5-HT 3 antagonists, such as mosapride, metoclopramide, renzapride, and zacopride, and so these compounds cannot be considered highly selective. Research in this area is ongoing. [11] Amongst these agonists prucalopride has >150-fold higher affinity for 5-HT4 receptors than for other ...
Certain prokinetic drugs such as cisapride, renzapride and metoclopramide, although not 5-HT 3 antagonists proper, possess some weak antagonist effect at the 5-HT 3 receptor. Galanolactone, a diterpenoid found in ginger, is a 5-HT 3 antagonist and is believed to at least partially mediate the anti-emetic activity of this plant.