Histamine is a monoamine signaling molecule that acts via four G-protein-coupled histamine receptors; H1, H2, H3 and H4. Histamine mediates numerous biological activities stimulated by various immunological and non-immunological stimuli, through differential expression of H1-4 on effector cells, such as mast cells and basophils.
Histamine Receptor Target Files
Histamine has a critical role in immumomodulation and allergic diseases. Other biological activities include cell proliferation, differentiation, hematopoiesis, embryonic development, regeneration, wound healing, aminergic neurotransmission, secretion of pituitary hormones and regulation of gastrointestinal and circulatory functions. The table below summarizes the properties of the histamine receptor subtypes.
|Localization||CNS, smooth muscle from airways, gastrointestinal tract, genitourinary system, and the cardiovascular system, adrenal medulla, endothelial cells, lymphocytes||Stomach, uterus, vascular smooth muscle, neutrophils, heart, CNS||CNS, peripheral nerves, heart, lungs, gastrointestinal tract, endothelial cells||Bone marrow and leukocytes|
|Likely Physiological Roles||Smooth muscle contraction, food intake, sleep-wakefulness||Gastric acid secretion, smooth muscle relaxation, modulation of the sinua rhythm||Presynaptic autoreceptors||Mast cell chemotaxis|
|Example Histamine Receptor Agonists||
VUF 8430 (2494)
|Example Histamine Receptor Antagonists||
ROS 234 (2034)
JNJ 10191584 (2441)
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Potent, selective LRRK2 inhibitor
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