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.