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  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • Consistent with the known mechanism of action of hallucinogens in humans, the behavioral effects of hallucinogens in rodents are mediated primarily by activation of 5-HT 2A receptors. (springer.com)
  • 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)
  • 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)
  • efficacy
  • Acuña-Castillo C, Villalobos C, Moya PR, Sáez P, Cassels BK, Huidobro-Toro JP (2002) Differences in potency and efficacy of a series of phenylisopropylamine/phenylethylamine pairs at 5-HT 2A and 5-HT 2C receptors. (springer.com)
  • 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)
  • 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)
  • 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)
  • 1997
  • Aghajanian GK, Marek GJ (1997) Serotonin induces excitatory postsynaptic potentials in apical dendrites of neocortical pyramidal cells. (springer.com)
  • 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)
  • 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)
  • therapeutic
  • 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)
  • Research in this area has been limited due to the cardiotoxicity of 5-HT2B agonists, and the lack of clear therapeutic application for 5-HT2B antagonists, but there is still a need for selective ligands for scientific research. (wikipedia.org)
  • characterization
  • Here we report the construction and characterization of a highly constitutive active H3 receptor (MT6), in which the 357 alanine residue was converted to lysine (A357K). (aspetjournals.org)
  • neuronal
  • 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)
  • effects
  • 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)
  • Other 5-HT2A agonists like LSD also have potent anti-inflammatory effects against TNF-alpha-induced inflammation. (wikipedia.org)
  • These data strongly suggest that the effects of high concentrations of α-me-5-HT are probably non-specific. (physoc.org)
  • Antidepressants, particularly those that affect serotonin metabolism, are famous for causing "sexual side effects. (blogspot.fi)
  • And finally: It's thought by some that Minoxidil owes its hair-regrowing effects to the fact that it's a nitric-oxide agonist (Mi-NO-xidil). (blogspot.fi)
  • Its negative effects such as anxiety, headaches, and appetite loss are likely mediated by its actions on the 5-HT2C receptor. (wikipedia.org)
  • It is known to have partial agonist effects on some of the other 5-HT receptors as well. (wikipedia.org)
  • It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. (wikipedia.org)