R&D Systems Inc. Tocris Bioscience Boston Biochem

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

Related Categories

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)

Quick Order

Find multiple products by catalog number

divider line

Histamine Review

Histamine Review

Written by Iwan de Esch and Rob Leurs, leading experts. Request a copy or view PDF today.

divider line

7-TM Receptor Signaling

Written by T. Kenakin et al

7-TM Poster

'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

divider line

New Therapies and Challenges in Asthma

Written by Peter J. Barnes

Asthma Poster

'New Therapies, Challenges, and Breakthroughs in Asthma' highlights key pathways and new therapies used to treat asthma, including those currently in clinical development.

divider line

New Product Guide

NPG

Highlights over 130 new products added in the second half of 2013. Request a copy or view PDF today.

divider line

Twitter Updates

Follow @Tocris on Twitter

Follow us on Twitter!

Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.