serotonin 2C receptor agonistSummary This chapter discusses the pharmacology, structure-activity relationship (SAR), pharmacokinetics and drug metabolism, efficacy and safety, and syntheses of lorcaserin. Fenfluramine works as an anti-obesity agent by modulating the serotonin level of the patient ...
The serotonin receptor subtype, 5-HT2A, is a G protein-coupled receptor expressed in multiple regions of the body e.g. gastrointestinal tract, liver, smooth muscles and platelets. It is also expressed in many areas of the central nervous system, which include the cortex and hippocampus1,2,3...
acidtryptophanby tryptophan-hydroxylase-1, expressed in the GI tract.4Upon its release, serotonin can exert effects through actions on 14 different identified receptors and is inactivated through the serotonin reuptake transporter system.1,3In the GI tract, the 5-HT4receptor is a key target.3,5...
Nair and Gudelsky (2004) demonstrated that systemic administration of a 5-HT2A/2C, 5-HT2, or 5-HT2C agonist results in an increase in prefrontal ACh release, and these increases are blocked by the administration of serotonin receptor antagonists. Agonists at 5-HT4 or 5-HT1A receptors also...
Among these metabolites, acetate upregulated the expression of free fatty acid receptor 3 and TPH1 while downregulated indoleamine 2,3-dioxygenase 1. Similar effects were also recapitulated when treating the cells with AR420626, an agonist targeting free fatty acid receptor 3. Conclusions Overall, ...
anatomically discrete. The radioligand used may also affect receptor binding since antagonist but not agonist binding is decreased in MDD, suggesting binding differences may reflect the G-protein coupled or uncoupled state of the receptor53. Lower 5-HT1Areceptor binding is reported in the cerebral ...
The demonstrated efficacy of clozapine in PDP has been attributed to serotonin (5-HT(2A)) receptor blockade. We postulated that pimavanserin (ACP-103), a highly selective 5-HT(2A) inverse agonist, would attenuate psychosis in patients with PDP, but avoid motoric worsening and non-motoric ...
, a selective 5-HT(2A/2C) receptor agonist. In the frontal cortex, 5-HT-mediated phospholipase C (PLC) enzyme activity decreased by 24 to 30% after 4 to 7 days of (-)-DOI treatment without any significant changes in the guanosine 5'-3-O-(thio)triphosphate-mediated PLC enzyme ...
The key outcome of 5-HT 2C receptor editing is downregulation of constitutive and agonist-stimulated receptor activity. This is due to the substantially decreased basal and agonist-stimulated G protein-coupling efficiency, decreased agonist affinity, and 5-HT potency as well as coupling of different...
serotonin receptor agonist and antagonist; antidepressant, anxoilytic agent, neurodegenerative diseases; neurodegenerative disease, cognition disorders, irritable bowel syndrome, nausea; 6,7-Dihydro-4-hydroxy-7-isopropyl-6-oxo-N-(3-(piperidin-1-yl)propyl)thieno[2,3-b]pyridine-5-carboxamid potassium ...