Histamine Plays an Important Role in Promoting and Stabilizing Wakefulness1-3
In the brain, histamine acts as a key wake-promoting neurotransmitter1,4
- Histamine is synthesized in the presynaptic neuron1
- When released into the synapse, histamine binds to postsynaptic H1 receptors1
Histamine neuronal activity in the brain is modulated by H1 and H3 receptors1
- H1 receptors increase neuronal activity, which allows for communication with brain regions that are important for sleep and wakefulness1-3
- H3 receptors are found primarily in the brain and help regulate histamine synthesis and release1,5-7
- Normally, when histamine levels in the brain are high, histamine binds to presynaptic H3 autoreceptors to inhibit further synthesis and release of histamine in the brain1,5