• cerebral cortex
  • Analysis of saturation binding data from Spontaneously Hypertensive Rat cerebral cortex indicate that as animals aged from six to sixteen weeks the maximal number of receptor sites (B max ) increased whereas the affinity of [ 3 H]-N-a-methylhistamine for these sites decreased. (tnstate.edu)
  • High performance liquid chromatography (HPLC) was used to determine brain histamine levels in the cerebral cortex. (tnstate.edu)
  • Histamine release in the brain triggers secondary release of excitatory neurotransmitters such as glutamate and acetylcholine via stimulation of H1 receptors in the cerebral cortex. (wikipedia.org)
  • Histamine has an excitatory effect in the brain via H1 receptors in the cerebral cortex, and so drugs such as ciproxifan which block the H3 receptor and consequently allow more histamine to be released have an alertness-promoting effect. (wikipedia.org)
  • ciproxifan
  • Ciproxifan produces wakefulness and attentiveness in animal studies, and produced cognitive enhancing effects without prominent stimulant effects at relatively low levels of receptor occupancy, and pronounced wakefulness at higher doses. (wikipedia.org)
  • therapeutic
  • There is a lot of interest in the histamine H3 receptor as a potential therapeutic target because of its involvement in the neuronal mechanism behind many cognitive H3R-disorders and especially its location in the central nervous system. (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)
  • mechanism
  • The functions of HA in the SNr include motor control via HA H3 receptors (H3Rs), although the mechanism remains far from elucidated. (ox.ac.uk)
  • Furthermore, by the mechanism of our proposed feedback model, we conclude that histamine release is dependent on the enhancement of control of the histamine H 3 receptor as an autoregulator. (tnstate.edu)
  • binds
  • Astemizole is rapidly absorbed from the gastrointestinal tract and competitively binds to histamine H1 receptor sites in the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. (wikipedia.org)
  • activation
  • Constitutive activation of histamine H3 receptor is recently documented in in vivo as well as in recombinant receptor systems in vitro. (aspetjournals.org)
  • Activation of the H1 receptor results in elevated levels of inositol phosphate through coupling to the Gq protein. (axonmedchem.com)
  • Activation of the H4 receptor in primary cells appears to be mainly coupled to pertussis-toxin-sensitive Gi/o proteins, which signal through increases in intracellular calcium. (axonmedchem.com)
  • In our experiments, activation of the H1R receptors was linked to the PLC pathway and Ca 2+ release from intracellular stores. (jneurosci.org)
  • brain
  • Furthermore, the propylene, butylene and pentylene homologues can discriminate between the two functional H3 receptor models in the guinea pig jejunum and mouse brain. (aspetjournals.org)