H1 receptor

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histamine receptor H1
Other data
LocusChr. 3 p25

The histamine H1 receptor is an important target for clinically important drugs, and is likely one of the most important receptors for modulating mammalian circadian cycles.

Histamine H1 receptor are metabotropic G-protein-coupled receptors expressed throughout the body, specifically in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. The H1 receptor is linked to an intracellular G-protein (Gq) which activates phospholipase C and the phosphatidylinositol (PIP2) signalling pathway.

H1 receptor and inflammation

The production of prostaglandin E2 synthase induces the release of histamine from neurons, consequentially causing systemic vasodilation, along with increased cell permeability due to the its action on H1 receptors.


Histamine H1 receptors are activated by endogenous histamine, which is released by neurons which have their cell bodies in the tuberomamillary neurons of the hypothalamus. The histaminergic neurons of the tubero-mammillary nucleus become active during the 'wake' cycle, firing at approximately 2Hz; during slow wave sleep this firing rate drops to approximately 0.5Hz. Finally during REM sleep, histaminergic neurons stop firing all together. It has been reported that histaminergic neurons have the most wake-selective firing pattern of all known neuronal types.[1]

In the cortex, activation of H1 receptors leads to inhibition of cell membrane potassium channels. This depolarizes the neurons and increases the resistance of the neuronal cell membrane, bringing the cell closer to its firing threshold and increasing the excitatory voltage produced by a given excitatory current. H1 receptor antagonists, or antihistamines, produce drowsiness because they oppose this action, reducing neuronal excitation.[2]

H1-receptor antagonists

see Antihistamine - H1-receptor antagonists


  1. Passani, M. B., Lin, J. S., Hancock, A., Crochet, S., Blandina, P., 2004. The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders. Trends Pharmacol Sci 25, 618-625.
  2. Reiner P. B., Kamondi A., 1994. Mechanisms of antihistamine-induced sedation in the human brain: H1 receptor activation reduces a background leakage potassium current. Neuroscience 59(3), 579-88.

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