Histamine receptor antagonists

Of the four members of the histamine receptor superfamily, the H3 is predominately expressed in the brain, localizing to cerebral cortex, amygdala, hippocampus, striatum, thalamus, and hypothalamus. H3 receptors are localized presynaptically on histaminergic nerve terminals and act as inhibitory autoreceptors; thus, when activated by histamine, histamine release and biosynthesis are blocked.38 Of relevance to AD, H3 receptors expressed on nonhistaminergic nerve terminals can modulate the release of ACh, DA, g-amino-butyric acid (GABA), glutamate, and serotonin. Thus, H3-receptor antagonists or inverse agonists, by blocking the inhibitory effects of histamine, will facilitate the release of multiple neurotransmitters, reminiscent of the effects of nAChR activation. H3-receptor antagonists enhance vigilance, promoting wakefulness in rats, mice, and cats, and improve cognitive function in a variety of preclinical models. H3-receptor inverse agonists are thus being targeted as therapeutics for AD and attention-deficit hyperactivity disorder. Prototypic H3-receptor antagonists include thioperamide 18 and ciproxifan 19. Newer H3-receptor antagonists include ABT-239 20, JNJ-5207852 21, and BF 2649 22.

Blood Pressure Health

Blood Pressure Health

Your heart pumps blood throughout your body using a network of tubing called arteries and capillaries which return the blood back to your heart via your veins. Blood pressure is the force of the blood pushing against the walls of your arteries as your heart beats.Learn more...

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