• agonists
  • 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)
  • Other 5-HT2A agonists like LSD also have potent anti-inflammatory effects against TNF-alpha-induced inflammation. (wikipedia.org)
  • 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)
  • In similar manner, older dopamine agonists used for Parkinson's disease such as bromocriptine and cabergoline are poorly selective for one dopamine receptor over another, and, although most of these agents do act as D2 agonists, they affect other subtypes as well. (wikipedia.org)
  • adenosine
  • 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)
  • The cumulative data indicate that adenosine, acting via A1 receptors, inhibits the cortically projecting cholinergic neuronal arousal system found in this basal forebrain region. (harvard.edu)
  • release serotonin
  • The temporal relationship between the emetogenic action of emetogenic drugs and the release of serotonin, as well as the efficacy of antiemetic agents suggest that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. (drugbank.ca)
  • Specifically, there are swellings, called varicosities , along the axon that release serotonin into the extraneuronal space. (encyclopedia.com)
  • ligands
  • Several selective D2 ligands are, however, now available, and this number is likely to increase as further research progresses. (wikipedia.org)
  • anticholinergic
  • They include: Cyproheptadine blocks 5-HT2A, H1 and is a mild anticholinergic. (wikipedia.org)
  • 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)
  • nausea
  • The 5-HT3 antagonists are also indicated in the prevention and treatment of radiation-induced nausea and vomiting (RINV), when needed, and postoperative nausea and vomiting (PONV). (wikipedia.org)
  • Clinical trials suggest that it is more effective than other 5-HT3 antagonists in preventing delayed CINV (nausea and vomiting that occur more than 24 hours after the first dose of chemotherapy). (wikipedia.org)
  • The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting. (drugbank.ca)
  • increases
  • Activation of the 5-HT2A receptor in hypothalamus causes increases in hormonal levels of oxytocin, prolactin, ACTH, corticosterone, and renin. (wikipedia.org)
  • molecular
  • Thus the 5-HT2 receptor family is composed of three separate molecular entities: the 5-HT2A (formerly known as 5-HT2 or D), the 5-HT2B (formerly known as 5-HT2F) and the 5-HT2C (formerly known as 5-HT1C) receptors. (wikipedia.org)
  • neurons
  • In contrast, in the central nervous system serotonin can also be synthesized by the neurons of the Raphe nuclei that are distributed along the length of the brainstem in nine pairs. (encyclopedia.com)
  • From there, serotonin can be diffused to activate special receptors that exist on the dendrites, the cell bodies, and the presynaptic terminals of the adjacent neurons. (encyclopedia.com)
  • Inflammatory
  • The Fc region of immunoglobulin E (IgE) becomes bound to mast cells and basophils and when IgE's paratopes bind to an antigen, it causes the cells to release histamine and other inflammatory mediators. (wikipedia.org)
  • morphine
  • Serotonin receptors were split into two classes by Gaddum and Picarelli when it was discovered that some of the serotonin-induced changes in the gut could be blocked by morphine, whilst the remainder of the response was inhibited by dibenzyline leading to the naming of M and D receptors respectively. (wikipedia.org)