Histamine receptors in the central nervous system

Abstract

The role of histamine in brain function is discussed. A brief review is presented on the three types of histamine receptors with regard to their biochemistry and functions, as well as on specific ligands, both agonists and antagonists. It is concluded that several aspects of the pharmacology of histamine in the central nervous system are still a matter of empirism and speculations. The recent publications on the brain-penetrating H2 antagonist zolantidine and the selective H3 agonists and antagonists are expected to contribute to the knowledge of the histaminergic pathways in the brain. Therapeutical areas within the central nervous system are related to behaviour (including wake-sleep), neuroendocrinal processes, the control of muscle activity and cerebral circulation.

Striatal cholinergic interneuron regulation and circuit effects

“…These receptors are widely expressed, but only H1, H2, and H3 are highly expressed in the striatum, with H1 and H2 expressed on ChIs, and the autoreceptor H3 being expressed presynaptically on HA-ergic terminals. H1 and H2 are excitatory, coupling to G q and G s respectively, while the inhibitory H3 receptor is coupled with G i (Timmerman, 1989 ; Haas et al, 2008 ). HA application has the net result of depolarization of ChIs, presumably acting through by H1 receptors (Bell et al, 2000 ).…”

Antihistamines indicated for systemic and topical treatment

“…Primárně je vazbou histaminu na H1 histaminový receptor popisováno ovlivnění funkcí centrálního nervového systému, jako je regulace cirkadiánních rytmů (spánek a bdění), ovlivnění energetické a endokrinní homeostázy, agresivity, vnímání bolesti, kognice a paměti, a má antikonvulzivní aktivitu (1,2,3). Na úrovni periferie majo- Článek přijat k publikaci: 12.…”

Die Innenohrdurchblutung unter Betahistin - Eine tierexperimentelle Studie1,2,3

“…Aequamen®, Vasomotal® oder Betaserc®) werden heute auf em duales pharmakologisches Wirkprinzip zurOckgefiihrt (1,7,31,32,34). Danach erfolgt einmal em agonistischer Angri ff von B an postsynaptischen Histaminrezeptoren vom Hi--Hydrogen clearance -HI -Typ, der zu einer verbesserten Jnnenohrdurchblutung fhhrt.…”

“…Simultan dazu greift B antagonistisch an den prdsynaptischen Histarninrezeptoren vom H3-Typ an, die in den vestibuldren Nuclei des ZNS lokalisiert sind. Vermutlich wird die Schwere und Frequenz der Schwindeiattacken dadurch reduziert(32,34). Die Nebenwirkungen des B auf den systemischen Blutdruck sowie die sedierende Wirkung werden als geringfiigig eingcschätzt (7).…”