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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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Histamine Review
Written by Iwan de Esch and Rob Leurs, leading experts. Request a copy or view PDF today.
7-TM Receptor Signaling
Written by T. Kenakin et al
'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy
New Therapies and Challenges in Asthma
Written by Peter J. Barnes
'New Therapies, Challenges, and Breakthroughs in Asthma' highlights key pathways and new therapies used to treat asthma, including those currently in clinical development.
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