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
Literature
Receptor Data

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.

Literature for Histamine Receptors

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Histamine Receptors

Histamine Receptors Scientific Review

Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.

Asthma

Asthma Poster

Asthma is one of the most common chronic diseases in the world, affecting over 300 million people. This poster highlights key pathways and new therapies used to treat the condition, including those currently in clinical development.

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.