Histamine Receptors

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

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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.

Receptor Subtype H1 H2 H3 H4
G protein Gq/11 Gs Gi/o Gi/o
Transduction Mechanism ↑PLC ↑cAMP ↓cAMP ↓cAMP
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 HTMT (0646)
2-Pyridylethylamine (2478)
Amthamine (0668)
Dimaprit (0506)
Imetit (0729)
Immepip (0932)
Immethridine (2315)
R-(-)-α-Methylhistamine (0569)
Methimepip (2947)
Clobenpropit (0752)*
Imetit (0729)
Immepip (0932)
4-Methylhistamine (2342)
VUF 8430 (2494)
Example Histamine Receptor Antagonists Clemastine (1453)
Fexofenadine (2429)
Mepyramine (0660)
Triprolidine (0662)
Cetirizine (2577)
Diphenhydramine (3072)
Aminopotentidine (0721)
Cimetidine (0902)
Ranitidine (1967)
Tiotidine (0826)
Zolantidine (1070)
Clobenpropit (0752)
Iodophenpropit (0779)
Thioperamide (0644)
ROS 234 (2034)
Thioperamide (0644)
JNJ 10191584 (2441)

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