• neurotransmitters
  • 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)
  • The H3 receptor has also been shown to presynaptically inhibit the release of a number of other neurotransmitters (i.e. it acts as an inhibitory heteroreceptor) including, but probably not limited to dopamine, GABA, acetylcholine, noradrenaline, histamine and serotonin. (wikipedia.org)
  • The interaction between histamine (H3-receptor) and dopamine as well as other neurotransmitters is an important underlying mechanism behind the disorder. (wikipedia.org)
  • More importantly, betahistine has a powerful antagonistic effects at H3 receptors, thereby increasing the levels of neurotransmitters histamine, acetylcholine, norepinephrine, serotonin, and GABA released from the nerve endings. (wikipedia.org)
  • Consequently
  • Consequently, cipralisant was reassessed as an H3 receptor agonist in human and rat recombinant systems, showing functional selectivity and stimulating one type of G-protein coupled pathway while failing to activate other intracellular pathways. (wikipedia.org)
  • Mechanism
  • 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)
  • weak
  • While all chiral analogues proved to be weak H1R antagonists, an achiral keto derivative of histaprodifen turned out to be the first 2-acylated histamine congener displaying partial H1R agonism. (uni-regensburg.de)
  • effects
  • Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice. (wikipedia.org)
  • decreases
  • Malmlöf K, Golozoubova V, Peschke B, Wulff BS, Refsgaard HH, Johansen PB, Cremers T, Rimvall K. Increase of neuronal histamine in obese rats is associated with decreases in body weight and plasma triglycerides. (wikipedia.org)
  • Mouse-models and other research demonstrated that reducing histamine concentration in the H3R causes tics, but adding histamine in the striatum decreases the symptoms. (wikipedia.org)
  • brain
  • The wide variety of potential pathophysiology of H3R in brain disorders makes H3R antagonists interesting for drug development. (wikipedia.org)
  • target
  • 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)
  • In view of this blockbuster status of the H1R and H2R antagonists, current expectations for the therapeutic potential of drugs that target the H3 and H4 receptors are high. (uni-regensburg.de)