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Bertlich, Mattis; Ihler, Friedrich; Freytag, Saskia; Weiss, Bernhard G.; Strupp, Michael und Canis, Martin (2015): Histaminergic H3-Heteroreceptors as a Potential Mediator of Betahistine-Induced Increase in Cochlear Blood Flow. In: Audiology & neuro-otology, Bd. 20, Nr. 5: S. 283-293 [PDF, 410kB]

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Abstract

OBJECTIVE Betahistine is a histamine-like drug that is considered beneficial in Ménière's disease by increasing cochlear blood flow. Acting as an agonist at the histamine H1-receptor and as an inverse agonist at the H3-receptor, these receptors as well as the adrenergic \textgreeka2-receptor were investigated for betahistine effects on cochlear blood flow. MATERIALS AND METHODS A total of 54 Dunkin-Hartley guinea pigs were randomly assigned to one of nine groups treated with a selection of H1-, H3- or \textgreeka2-selective agonists and antagonists together with betahistine. Cochlear blood flow and mean arterial pressure were recorded for 3 min before and 15 min after infusion. RESULTS Blockage of the H3- or \textgreeka2-receptors caused a suppression of betahistine-mediated typical changes in cochlear blood flow or blood pressure. Activation of H3-receptors caused a drop in cochlear blood flow and blood pressure. H1-receptors showed no involvement in betahistine-mediated changes of cochlear blood flow. CONCLUSION Betahistine most likely affects cochlear blood flow through histaminergic H3-heteroreceptors.

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