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.
Targets
Histamine Receptor Target Files
Histamine H1 Receptors (Histamine H1 R) | Histamine H3 Receptors (Histamine H3 R) |
Histamine H2 Receptors (Histamine H2 R) | Histamine H4 Receptors (Histamine H4 R) |
Related Targets
Histamine has a critical role in immunomodulation 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.
Receptor Data
Histamine Receptor Data
| 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 Agonists | HTMT (0646) 2-Pyridylethylamine (2478) | Histamine (3545) HTMT dimaleate (0646) | Imetit (0729) Immepip (0932) Histamine (3545) | Clobenpropit (0752)* Imetit (0729) Immepip (0932) 4-Methylhistamine (2342) |
| Example Antagonists | Clemastine (1453) Diphenhydramine (3072) Meclizine (4245) Olopatadine (4241) Terfenadine (3948) | Tiotidine (0826) Zolantidine (1070) | Clobenpropit (0752) Thioperamide (0644) JNJ 5207852 (4020) | Thioperamide (0644) JNJ 10191584 (2441) JNJ 7777120 (4021) JNJ 39758979 (6279) |
* Displays partial agonist effects
References
Leurs and Timmmerman (1997) Histamine receptors. Tocris Reviews. No. 6. Hill et al (1997) Internation union of pharmacology. XIII. Classification of histamine receptors. Pharmacol.Rev. 49 253. Leurs et al (2001) Histamine receptors are finally 'coming out'. TiPS 22 337. Schneider et al (2002) Trends in histamine research: new functions during immune responses and hematopoiesis. Trends Immunol. 23 255.