Actions of betahistine at histamine receptors in the brain
References (45)
- et al.
Distribution and characteristics of histamine H1-receptors in guinea-pig airways identified by [3H]mepyramine
European J. Pharmacol.
(1982) Chemistry and structure-activity relationships of drugs acting at histamine receptors
- et al.
Effects of kainic acid on histaminergic systems in guinea-pig hippocampus
Brain Res.
(1978) - et al.
Central actions of histmine: microelectrophoretic studies
Brain Res.
(1977) Histamine receptors and cyclic nucleotides
- et al.
Protein measurements with the Folin phenol reagent
J. Biol. Chem.
(1951) - et al.
In vivo occupation of cerebral histamine H1-receptors evaluated with [3H]mepyramine may predict sedative properties of psychotropic drugs
European J. Pharmacol.
(1979) - et al.
Labeling of histamine H1-receptors in the brain of the living mouse
Neurosci. Lett.
(1980) Histamine receptors in brain
Life Sci.
(1979)- et al.
Histamine receptors in the brain and their possible functions
A sensitive method of glycogen determination in the presence of interfering substances utilizing the filter-paper technique
Anal. Biochem.
Effects of betahistine HCl, nicotinic acid and histamine on basilar blood flow in anesthetized dogs
Stroke
Autoinhibition of brain histamine release mediated by a novel class (H3) of histamine receptor
Nature
Autoregulation of histamine release in brain by presynaptic receptors
Neuroscience
The subcellular localisation of histidine decarboxylase in various regions of rat brain
J. Neurochem.
A simple and sensitive saturation assay method for the measurement of adenosine 3′,5′-cyclic monophosphate
Biochem. J.
Histamine H1-receptors binding sites in guinea-pig brain membranes: regulation of agonist interactions by guanine nucleotides and cations
J. Neurochem.
Heterogeneity of histamine H1-receptors: species variations in [3H]mepyramine binding of brain membranes
J. Neurochem.
Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an e enzymatic reaction
Biochem. Pharmacol.
Pharmacological specificity of brain histamine H2-receptors differs in intact cells and cell-free preparations
Nature
Histamine H1-agonist potentiation of adenosine-stimulated cyclic AMP accumulation in slices of guinea-pig cerebral cortex: comparison of responses and binding parameters
Br. J. Pharmacol.
Impromidine (SK & F 92676) is a very potent and specific agonist for histamine H2 receptors
Nature
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Drug repurposing: Clemastine fumarate and neurodegeneration
2023, Biomedicine and PharmacotherapyCitation Excerpt :H2 receptor antagonists have been broadly used in gastric ulcer treatment [6]. Histamine-3 receptors are autoreceptors that sit in histaminergic neurons and regulate the production and/or release of histamine as a part of negative feedback loop, as well as heteroreceptors that sit in non-histaminergic neurons and block the release of a variety of other neurotransmitters such as serotonin, norepinephrine, acetylcholine, and dopamine [7-11]. Histamine-4 receptors engaging in eosinophil shape change and mast cell chemotaxis [12,13], whose blockage is possibly beneficial to reducing microglia-meditated inflammation [14].
Current and Emerging Medical Therapies for Dizziness
2021, Otolaryngologic Clinics of North AmericaCitation Excerpt :Side effects include hypersomnolence, dry mouth, and urinary retention.14 Betahistine is a histamine analogue with antagonistic effects on H3 receptors and partial agonist effects on H1 and H2 receptors.15,16 It is thought to reduce the incidence and severity of vertigo, nausea, and emesis through changes in inner ear blood flow.17
Psychotomimetic-like behavioral effects of memantine in the mouse
2018, Biomedicine and PharmacotherapyCitation Excerpt :Secondly, we investigated effects of haloperidol, a dopamine D2 receptor antagonist, on memantine-induced stereotyped behaviors, since haloperidol blocks METH-induced stereotypy [23]. Betahistine (2-[2-(methylamino)ethyl]pyridine) is an agent used in the treatment of vertigo associated with Ménière's disease [24], which is an analogue of histamine with weak agonist properties at histamine H1 receptors and more potent antagonistic effects at histamine H3 receptors [25], consequently increasing histamine turnover and releasing histamine in the brain [26]. The effect of betahistine on memantine-induced stereotypy was investigated as drugs with similar actions on histamine suppress METH-induced stereotypy since stereotypies induced by METH are alleviated by the brain histamine degrading enzyme (i.e. histamine N-methyltransferase) inhibitors, agents which increase histamine contents in the brain [27].