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Small Molecules
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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) |
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 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) |
* 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.