Histamine H3 receptor antagonists – Roles in neurological and endocrine diseases and diabetes mellitus - 27/05/22
Abstract |
Human histamine H3 receptor (H3R) was initially described in the brain of rat in 1983 and cloned in 1999. It can be found in the human brain and functions as a regulator of histamine synthesis and release. H3 receptors are predominantly resident in the presynaptic region of neurons containing histamine, where they modulate the synthesis and release of histamine (autoreceptor) or other neurotransmitters such as dopamine, norepinephrine, gamma-aminobutyric acid (GABA), glutamate, acetylcholine and serotonin (all heteroreceptors). The human histamine H3 receptor has twenty isoforms of which eight are functional. H3 receptor expression is seen in the cerebral cortex, neurons of the basal ganglia and hippocampus, which are important for process of cognition, sleep and homoeostatic regulation. In addition, histamine H3R antagonists stimulate insulin release, through inducing the release of acetylcholine and cause significant reduction in total body weight and triglycerides in obese subjects by causing a feeling of satiety in the hypothalamus. The ability of histamine H3R antagonist to reduce diabetes-induced hyperglycaemia is comparable to that of metformin. It is reasonable therefore, to claim that H3 receptor antagonists may play an important role in the therapy of disorders of cognition, the ability to sleep, oxidative stress, inflammation and anomaly of glucose homoeostasis. A large number of H3R antagonists are being developed by pharmaceutical companies and university research centres. As examples of these new drugs, this review will discuss a number of drugs, including the first histamine H3R receptor antagonist produced.
Le texte complet de cet article est disponible en PDF.Graphical Abstract |
Highlights |
• | Histamine H3 receptor (H3R) antagonists can be used to treat sleeping disorders such as narcolepsy. |
• | Epilepsy and Parkinson diseases can be treated with histamine H3R antagonists. |
• | It reduces body weight and triglyceride level in obese subjects by inducing the feeling of satiety. |
• | Histamine H3R antagonists stimulate insulin release and reduce hyperglycaemia in a comparable manner to that of metformin. |
• | Histamine H3R receptor antagonists reduce inflammation and improve cognition via release of acetylcholine. |
Keywords : Histamine, Histamine receptor, Neurotransmitters, H3-receptor antagonists, Neurological diseases, Endocrine disorders, Diabetes mellitus, Pancreatic beta cell
Plan
Vol 150
Article 112947- juin 2022 Retour au numéroBienvenue sur EM-consulte, la référence des professionnels de santé.
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