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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)
  • 1997
  • Aghajanian GK, Marek GJ (1997) Serotonin induces excitatory postsynaptic potentials in apical dendrites of neocortical pyramidal cells. (springer.com)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • serotonergic
  • The development of 5-HT2C receptor knockout mice in the mid-1990s was a hallmark achievement in the identification and development of serotonergic drugs for weight loss. (wikipedia.org)
  • As a result of these symptoms, the researchers identified a functional role for the receptors in serotonergic regulation of food intake and body weight. (wikipedia.org)
  • This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD. (wikipedia.org)
  • The 5-HT 2A receptor appears to be the primary site of action with significant modulation by other serotonergic sites including 5-HT 2C and 5-HT 1A receptors. (springer.com)
  • Rats
  • WAY-163909 (10 mg/kg, i.p. or s.c.) decreased immobility time in Wistar-Kyoto rats in the FST, effects that were reversed by the 5-HT 2C/2B receptor antagonist SB 206553. (springer.com)
  • Administration of WAY-163909 (3 mg/kg, i.p.) for 5 or 21 days decreased the BULB-induced hyperactivity in rats. (springer.com)
  • Arnt J, Hyttel J (1989) Facilitation of 8-OHDPAT-induced forepaw treading of rats by the 5-HT2 agonist DOI. (springer.com)
  • Baladi MG, Newman AH, France CP (2010) Dopamine D3 receptors mediate the discriminative stimulus effects of quinpirole in free-feeding rats. (springer.com)
  • cannabinoid
  • This methodology was then applied to design and experimentally confirm structures of three mutants of the CB1 cannabinoid receptor associated with different functions. (pnas.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)
  • opioid
  • General Action and Information Opioids bind to opiate receptors in the CNS, where they act as agonists of endogenously occurring opioid peptides (eukephalins and endorphins). (cnsdiseases.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)
  • Novel
  • The present studies were conducted to evaluate the effects of the novel 5-HT 2C receptor agonist WAY-163909 in animal models of antidepressant activity (forced swim test (FST), resident-intruder, olfactory bulbectomy (BULB)), in a schedule-induced polydipsia (SIP) model of obsessive-compulsive disorder and in a model for evaluating sexual dysfunction. (springer.com)
  • Taken together, these results demonstrate that the novel 5-HT 2C receptor agonist WAY-163909 produces rapid onset antidepressant-like effects in animal models and may be a novel treatment for depression. (springer.com)
  • In 2014, a novel 5-HT receptor was isolated from the small white butterfly, Pieris rapae, and named pr5-HT8. (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)
  • concentrations
  • These data strongly suggest that the effects of high concentrations of α-me-5-HT are probably non-specific. (physoc.org)
  • blockade
  • They also found that exposing serotonin to a cell line expressing SERT and nNOS caused the production of NO . Thus, if you blockade SERT (cutting off serotonin reuptake), you interfere with NO production at the source, because nNOS (the enzyme responsible for producing NO) and SERT (the serotonin transporter) are, in fact, joined together, in vivo . (blogspot.fi)
  • Nicotinic
  • also a non-competitive antagonist of nicotinic acetylcholine receptors Amineptine (Survector, Maneon) and nomifensine (Merital, Alival) were also formerly marketed, but have since been withdrawn due to toxicity. (wikipedia.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)
  • syndrome
  • They include: Dolasetron Granisetron Ondansetron Palonosetron Tropisetron Other 5-HT3 antagonists are used for the treatment of irritable bowel syndrome: Alosetron Cilansetron Also, the antidepressant mirtazapine acts as a 5-HT3 antagonist. (wikipedia.org)
  • PCPA) An inhibitor of serotonin synthesis that has been used in the treatment of carcinoid syndrome. (wikipedia.org)
  • It may also be used in the treatment of serotonin syndrome. (wikipedia.org)