H3 receptor antagonists

thumb|260px|right|Betahistine(12mg) Betahistine, sold under the brand name Serc among others, is an anti-vertigo medication. It is commonly prescribed for balance disorders or to alleviate vertigo symptoms. It was first registered in Europe in 1970 for the treatment of Ménière's disease, but current evidence does not support its efficacy in treating it.

Pitolisant, sold under the brand name Wakix among others, is a medication used for the treatment of excessive daytime sleepiness in adults with narcolepsy. It is an inverse agonist of the histamine H3 receptor. It represents the first commercially available medication in its class, so that the U.S. Food and Drug Administration (FDA) declares it a first-in-class medication. Pitolisant enhances the activity of histaminergic neurons in the brain that function to improve a person's wakefulness. It was approved by the European Medicines Agency (EMA) in March 2016 for narcolepsy with or without cata

Burimamide is an antagonist at the H2 and H3 histamine receptors. At physiological pH, it is largely inactive as an H2 antagonist, but its H3 affinity is 100x higher. It is a thiourea derivative.

Conessine is a steroidal alkaloid found in a number of plant species from the family Apocynaceae, including Holarrhena floribunda, Holarrhena antidysenterica and Funtumia elastica. It acts as a histamine antagonist, selective for the H3 subtype (with an affinity of pKi = 8.27; Ki = ~5 nM). It was also found to have long CNS clearance times, high blood–brain barrier penetration and high affinity for the adrenergic receptors.

Impentamine is a histamine antagonist selective for the H3 subtype.

chemical compound

Iodophenpropit is a histamine antagonist which binds selectively to the H3 subtype. Its 125I radiolabelled form has been used for mapping the distribution of H3 receptors in animal studies.

SCH-79687 is a histamine antagonist selective for the H3 subtype.

Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist.

Clobenpropit is a histamine H3 receptor antagonist. It has neuroprotective effects via stimulation of GABA release in brain cells in vitro.