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  • Agonist
  • H 1 -antihistamines can also reduce inflammation, since the expression of NF-κB , the transcription factor the regulates inflammatory processes, is promoted by both the receptor's constitutive activity and agonist (i.e., histamine ) binding at the H 1 receptor. (wikipedia.org)
  • 1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane (0.3 mg/kg), a 5-HT 2A/2C agonist, shifted the methamphetamine dose-response curve to the left, and this leftward shift was antagonized by the coadministration of ketanserin (3.0 mg/kg), a 5-HT 2A/2C antagonist. (aspetjournals.org)
  • In contrast, tropisetron (1.0 mg/kg), a 5-HT 3 antagonist, produced a shift to the left of the methamphetamine dose-response curve, and this effect of tropisetron was antagonized by the coadministration of m -chlorophenyl-biguanide (1.8 mg/kg), a 5-HT 3 agonist. (aspetjournals.org)
  • Servier
  • To that aim, 14 month old C57/Bl6 mice were administered per oesophagy during nine consecutive days with Donepezil (at 0.1 and 0.3 mg/kg) and S 38093 (at 0.1, 0.3, and 1.0 mg/kg), a H3 histaminergic antagonist developed by Servier, alone or in combination and tested for memory in a contextual memory task that modelized the age-induced memory dysfunction. (frontiersin.org)
  • histaminergic
  • Moreover, the protective effect observed for ligand 14 in MES model was lower than that observed for the reference drug phenytoin and was entirely abrogated when rats were co-administered with the brain-penetrant H1R antagonist pyrilamine (PYR) but not the brain-penetrant H2R antagonist zolantidine (ZOL), demonstrating that histaminergic neurotransmission by activation of postsynaptically located H1Rs seems to be involved in the protective action. (dovepress.com)
  • mast cells
  • Brain "fog" may be due to inflammatory molecules, including adipocytokines and histamine released from mast cells (MCs) further stimulating microglia activation, and causing focal brain inflammation. (frontiersin.org)
  • gastric
  • Antagonists that target H1R or H2R and are used in the treatment of allergic conditions, such as rhinitis, or of gastric acid release disorders, have been �blockbuster� drugs for many years. (uni-regensburg.de)
  • Antihistamines that target the histamine H 2 -receptor are used to treat gastric acid conditions (e.g., peptic ulcers and acid reflux ). (wikipedia.org)
  • work
  • Verongamine is a specific histamine-H3 antagonist at concentrations as low as 1 microgram/ml.This document is the accepted manuscript version of a published work that appeared in final form in Journal of Natural Products after peer review and technical editing by the publisher. (duhnnae.com)
  • shown
  • It has been shown that attempts to rigidize flexible H3R antagonists, such as FUB-372 and/or iodoproxyfan, have ultimately led to a more or less severe attenuation of H3R affinity. (uni-regensburg.de)