Histamine H3 Receptors
Histamine H3 receptors are Gαi/o-protein-coupled receptors expressed at high levels on histaminergic neurons in the CNS, particularly in the basal ganglia, cortex and hippocampus. H3 receptors are thought to function as presynaptic autoreceptors.
Histamine H3 Receptor Agonists |
|
|---|---|
| Cat. No. | Product Name / Activity |
| 3545 | Histamine dihydrochloride |
| Endogenous histamine receptor agonist | |
| 0729 | Imetit dihydrobromide |
| Standard H3 and H4 agonist (H3 > H4) | |
| 0932 | Immepip dihydrobromide |
| Standard H3 agonist. Also H4 agonist | |
| 2315 | Immethridine dihydrobromide |
| Potent H3 agonist, highly selective over H4 | |
| 0569 | (R)-(-)-α-Methylhistamine dihydrobromide |
| Potent, standard H3 agonist | |
Histamine H3 Receptor Inverse Agonists |
|
| Cat. No. | Product Name / Activity |
| 3743 | BF 2649 hydrochloride |
| Potent and selective H3 inverse agonist | |
Histamine H3 Receptor Antagonists |
|
| Cat. No. | Product Name / Activity |
| 0752 | Clobenpropit dihydrobromide |
| Highly potent H3 antagonist and H4 partial agonist | |
| 0779 | Iodophenpropit dihydrobromide |
| Potent, selective H3 antagonist | |
| 4020 | JNJ 5207852 dihydrochloride |
| High affinity H3 antagonist | |
| 6778 | S 38093 |
| Selective H3 antagonist and inverse agonist; also σ1 receptor antagonist; antinociceptive | |
| 0644 | Thioperamide |
| H3 antagonist; also H4 inverse agonist | |
Histamine H3 receptors are Gαi/o-protein-coupled receptors first cloned in 1999. H3 receptors are expressed at high levels on histaminergic neurons in the central nervous system, particularly in the basal ganglia, cortex, hippocampus and strial area. They are expressed in the periphery at lower densities in the gastrointestinal, bronchial and cardiovascular systems.
H3 receptors are thought to function as presynaptic autoreceptors and their activation stimulates the negative feedback mechanism that reduces central histaminergic activity. These receptors have displayed heterogeneity in binding and functional studies, suggesting multiple subtypes. In rats, three H3 receptor subtypes have been identified and they all vary in the length of the third extracellular loop, have distinct CNS localization and differentially couple to adenylyl cyclase and MAPK signaling pathways.
H3 receptors have multiple functions including roles in cognition, sleep-wake status, energy homeostasis regulation and inflammation. Activation of these receptors can inhibit histamine, dopamine, serotonin, noradrenalin and acetylcholine release and they participate in control of neurogenic inflammation through local-neuron feedback loops. Furthermore, H3 receptor activation increases antigen-presenting cell capacity.
H3 receptors are thought to have pathophysiological relevance and are involved in cognitive impairment, seizures and possibly metabolic syndrome. The human gene encoding this receptor is localized to chromosome 20q13.33.
External sources of pharmacological information for Histamine H3 Receptors :
Literature for Histamine H3 Receptors
Tocris offers the following scientific literature for Histamine H3 Receptors to showcase our products. We invite you to request* your copy today!
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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
- Glutamate Receptors
- Frizzled Receptors
- GPCR Signaling
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.
Alzheimer's Poster
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Our Histamine review gives an overview of the different histamine receptor subtypes, as well as highlighting pharmacological ligands for their study.
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Our Alzheimer's disease poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease.
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