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  • Pharmacology
  • Unlike most anxiolytics, the pharmacology of buspirone is not related to that of benzodiazepines, barbiturates, or carbamates (it is not a GABA receptor agonist), and so buspirone does not carry the risk of physical dependence and withdrawal symptoms for which those drug classes are known. (wikipedia.org)
  • partial agonists
  • Role in memory and learning Activation of the 5-HT2A receptor is necessary for the effects of the "classic" psychedelics like LSD, psilocin and mescaline, which act as full or partial agonists at this receptor, and represent the three main classes of 5-HT2A agonists, the ergolines, tryptamines and phenethylamines, respectively. (wikipedia.org)
  • inhibits
  • Dexfenfluramine inhibits serotonin reuptake, stimulating the release of serotonin. (wikipedia.org)
  • 5-Benzyloxytryptamine "In summary, results of our study indicated that BW723C86 inhibits melanin synthesis by suppressing the expression of melanogenesis-related proteins (tyrosinase, TRP-1, and TRP-2) at the transcriptional level. (wikipedia.org)
  • Activation
  • Activation of 5-HT2A receptors can induce hallucinations, and the activation of 5-HT2B receptors has been implicated in cardiac valvular insufficiency and possibly in pulmonary hypertension. (wikipedia.org)
  • There are many additional signal cascade components that include the formation of arachidonic acid through PLA2 activity, activation of phospholipase D, Rho/Rho kinase, and ERK pathway activation initiated by agonist stimulation of the receptor. (wikipedia.org)
  • citation needed] Physiological processes mediated by the receptor include: CNS: neuronal excitation (most likely responsible for the psychedelic effects associated with 5-HT2A receptor agonists such as LSD, DMT, etc.), behavioural effects, learning, anxiety smooth muscle: contraction (in bronchi and gastrointestinal tract) vasoconstriction / vasodilation platelets: aggregation Activation of the 5-HT2A receptor with 2,5-Dimethoxy-4-iodoamphetamine (DOI) produces potent anti-inflammatory effects in several tissues including cardiovascular and gut. (wikipedia.org)
  • Activation of the 5-HT2A receptor in hypothalamus causes increases in hormonal levels of oxytocin, prolactin, ACTH, corticosterone, and renin. (wikipedia.org)
  • Constitutive activation of histamine H3 receptor is recently documented in in vivo as well as in recombinant receptor systems in vitro. (aspetjournals.org)
  • Many neuromodulators affect the excitability of these neurones and specifically, serotonin (5-HT) may modulate these neurones via activation of 5-HT 2C receptors (Heisler et al. (physoc.org)
  • Surprisingly however 5-HT2B receptor activation appears to be protective against the development of serotonin syndrome following elevated extracellular serotonin levels, despite its role in modulating serotonin release. (wikipedia.org)
  • post-synaptic
  • These findings suggest that post-synaptic 5-HT2A overdensity is involved in the pathogenesis of depression. (wikipedia.org)
  • stimulation
  • 5-HT2 receptor stimulation causes a buildup of intracellular inositol triphosphate and thereby an increase of cytosolic Ca2+. (wikipedia.org)
  • Upon receptor stimulation with agonist, Gαq and β-γ subunits dissociate to initiate downstream effector pathways. (wikipedia.org)
  • The 5-HT2B receptor stimulation can also lead to pathological proliferation of cardiac valves fibroblasts, which with chronic overstimulation of 5-HT2B can lead to a severe valvulopathy. (wikipedia.org)
  • modulate
  • Especially high concentrations of this receptor on the apical dendrites of pyramidal cells in layer V of the cortex may modulate cognitive processes, working memory, and attention by enhancing glutamate release followed by a complex range of interactions with the 5-HT1A, GABAA, adenosine A1, AMPA, mGluR2/3, mGlu5, and OX2 receptors. (wikipedia.org)
  • 2005). To determine if 5-HT could modulate these neurones, whole cell current-clamp recordings were made from hypothalamic arcuate neurones (GFP positive) identified by epifluorescence and differential interference contrast microscopy, as previously described (Choudhury et al. (physoc.org)
  • These data suggest that 5-HT 1, 5, 6 or 7 receptors may modulate the 5-HT response in RipCre neurons. (physoc.org)
  • modulator
  • The human 5-hydroxytryptamine-2C (5-HT 2C ) receptor has been the target of potential anxiolytics and antiobesity drugs, and its positive allosteric modulator was discovered to be l - threo -α- d -galacto-octopyranoside, methyl-7-chloro-6,7,8-trideoxy-6-[[(4-undecyl-2-piperidinyl)carbonyl]amino]-1-thiomonohydrochloride (2 S - cis ) (PNU-69176E). (aspetjournals.org)
  • GPCRs
  • This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. (wikipedia.org)
  • G-protein-coupled receptors (GPCRs) play a major role in signal transduction and are the targets of a large number of therapeutic drugs. (aspetjournals.org)
  • Classical models of GPCRs require agonist occupation of receptors to activate signal transduction pathways. (aspetjournals.org)
  • This model has recently been extended to accommodate the observations that several GPCRs can activate G-proteins in the absence of agonists, and that mutations in different structural domains of the GPCRs can enhance the agonist-independent (constitutive) activities. (aspetjournals.org)
  • neurons
  • While POMC neurons synthesize and secrete an anorexigenic peptide, α-melanocyte-stimulating hormone (α-MSH), to activate melanocortin receptors, NPY/AgRP neurons release orexigenic peptides, NPY, and AgRP. (pubmedcentralcanada.ca)
  • To circumvent this issue and establish the role of NPY/AgRP neurons in the control of body weight, several groups have used distinct genetic mouse models to achieve selective ablation of NPY/AgRP neurons during adulthood. (pubmedcentralcanada.ca)
  • We tested the hypothesis that 5-HT promotes the differentiation of enteric neurons by stimulating a developmentally regulated receptor expressed by crest-derived neuronal progenitors. (jneurosci.org)
  • These data demonstrate for the first time that the 5-HT 2B receptor is expressed in the small intestine as well as the stomach and that it is expressed by enteric neurons as well as by muscle. (jneurosci.org)
  • 5-HT could thus influence the fate of late-developing neurons. (jneurosci.org)
  • Enterochromaffin cells (EC), which are by far the largest enteric source of 5-HT, also develop before the mash-1 -independent lineage of enteric neurons ( Branchek and Gershon, 1989 ). (jneurosci.org)
  • neuronal
  • The promotion of in vitro neuronal differentiation by 5-HT and DOI was blocked by the 5-HT 1/2 antagonist methysergide, the pan-5-HT 2 antagonist ritanserin, and the 5-HT 2B/2C -selective antagonist SB206553. (jneurosci.org)
  • 5-HT 2B -immunoreactive cells were found to be a subset of cells that expressed the neuronal marker PGP9.5. (jneurosci.org)
  • Application of 5-HT to the perfusion solution (1 μM) or ejection (2 μM) directly above the recording neurone had a mixed affect on neuronal excitability. (physoc.org)
  • 1 μM) failed to induce any changes in neuronal excitability (n = 5). (physoc.org)
  • pharmacological
  • Studies using pharmacological and genetic tools demonstrated that the 5-HT2C receptor subtype was one of the principal mediators through which serotonin exerts its anorectic effects in rodents. (wikipedia.org)
  • For other drug classes (e.g., opioids), a number of strategies are used to treat abuse, including agonist replacement therapies (e.g., methadone) and treatment with a pharmacological antagonist (e.g., naltrexone). (aspetjournals.org)
  • anxiolytic
  • It has anxiolytic effects in animal studies, and is also used for investigating the function of the 5-HT2B receptor in a range of other tissues. (wikipedia.org)
  • methysergide
  • Chlorpromazine Cyproheptadine Metergoline Methysergide Mianserin Mirtazapine Oxetorone Pizotifen Propranolol Ritanserin Spiperone Carbinoxamine Cyproheptadine Hydroxyzine Methdilazine Pizotifen Promethazine Pizotifen is a 5-HT2C antagonist, H1 blocker and anticholinergic useful in migraine prophylaxis. (wikipedia.org)
  • efficacy
  • For example, pre-clinical studies with G protein biased agonists at the mu opioid receptor show equivalent efficacy for treating pain with reduced risk for addictive potential and respiratory depression. (wikipedia.org)
  • The approval was based on efficacy demonstrated in 5 "adequate and well-controlled" clinical trials, including 4 short-term studies (4 or 6 weeks) showing a reduction in psychotic symptoms in the acute setting and 1 longer-term study (26 weeks) demonstrating reduced relapse compared to placebo. (wikipedia.org)
  • compounds
  • The 5-HT2c receptor agonist Fenfluramine (market names Pondimin, Ponderax and Adifax) was discovered in 1972 as a result of research performed to identify anorectic compounds lacking the effects of psycho-stimulants and sympathomimetic agents (such as amphetamines). (wikipedia.org)
  • such compounds may be termed as mixed agonist-antagonists. (wikipedia.org)
  • In this study, we searched for compounds that stimulate [ 3 H]5-HT binding, the seeming hallmark of positive allosteric modulators. (aspetjournals.org)
  • regulates
  • PLC metabolizes phosphatidylinositol 4,5-bisphosphate into inositol 1,4,5-triphosphate (IP3), which regulates cellular Ca2+ flux by binding to IP3 receptors, thereby inducing the release of Ca2+. (wikipedia.org)
  • The 5-HT2B receptor subtype is involved in: CNS: presynaptic inhibition, behavioural effects Vascular: pulmonary vasoconstriction Cardiac: The 5-HT2B receptor regulates cardiac structure and functions as demonstrated by the abnormal cardiac development observed in 5-HT2B receptor null mice. (wikipedia.org)
  • concentrations
  • These data strongly suggest that the effects of high concentrations of α-me-5-HT are probably non-specific. (physoc.org)
  • obesity
  • 5-HT2C receptor agonists are attractive drug targets that have potential use in the treatment of a number of conditions including obesity, psychiatric disorders, sexual dysfunction and urinary incontinence. (wikipedia.org)
  • Later, 5-HT2C receptors were proposed as a therapeutic target for the treatment of multiple central nervous system (CNS) disorders including: psychiatric disorders, obesity, sexual dysfunction and urinary incontinence. (wikipedia.org)
  • cardiac
  • The symptoms and the treatment of an overdose are largely the same as for the other TCAs, including the presentation of serotonin syndrome and adverse cardiac effects. (wikipedia.org)
  • It appears that the 5-HT2B receptors, expressed in cardiac valves, are responsible for the valvulopathies reported from the use of fenfluramine and dexfenfluramine. (wikipedia.org)
  • Moreover, 5-HT2B receptors were recently shown to be overexpressed in human failing heart and antagonists of 5-HT2B receptors were uncovered to prevent both angiotensin II or beta-adrenergic agonist-induced pathological cardiac hypertrophy in mouse. (wikipedia.org)
  • migraine
  • Alpha Antagonists The U.S. Headache Consortium Guidelines and the AHCPR Technical Review included 17 controlled trials of a2 agonists for the prevention of migraine: 16 of clonidine () and one of guanfacine. (cnsdiseases.com)