Histamine serves as the endogenous ligand for the class of G protein-coupled receptors known as histamine receptors. The H1 receptor, H2 receptor, H3 receptor, and H4 receptor are the four recognized histamine receptors. A member of the family of G-protein-coupled receptors that resemble Rhodopsin is the histamine receptor H1. This receptor, specifically expressed in smooth muscles, vascular endothelial cells, the heart, and the central nervous system, is triggered by the biogenic amine histamine and is found throughout the body. Gs mediates the positive coupling of H2 receptors to adenylate cyclase. It is a strong inducer of cAMP synthesis, which activates Protein Kinase A. Histamine H3 receptors act as autoreceptors in presynaptic histaminergic neurons and regulate histamine turnover by feedback inhibition of histamine synthesis and release. They are expressed in the central nervous system and to a lesser extent the peripheral nervous system. It has been demonstrated that the mast cell chemotaxis and eosinophil shape change are both mediated by the histamine H4 receptor.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V70380 | Proxibarbal (Proxibarbital) | 2537-29-3 | Proxibarbal is a barbiturate analogue. |
|
V70323 | Samelisant free base (SUVN-G3031 free base) | 1394808-82-2 | Samelisant (SUVN-G3031) free base is an orally bioavailable, BBB (blood-brain barrier)-passing, selective histamine H3 receptor (H3R) inverse agonist. |
|
V70359 | Sequifenadine | 57734-69-7 | Sequifenadine is an H1 antihistamine. |
|
V70343 | ST-1006 Maleate | 1196994-12-3 | ST-1006 maleate is a potent histamine H4 receptor agonist (activator) with pKi of 7.94. |
|
V70316 | Tesmilifene fumarate (DPPE fumarate) | 1185241-83-1 | Tesmilifene fumarate (DPPE fumarate) is an H1C receptor antagonist that can broadly enhance the cytotoxic effect of chemotherapy and protect normal cells. |
|
V70360 | Thioperamide maleate (MR-12842 maleate) | 148440-81-7 | Thioperamide maleate (MR-12842 maleate) is a potent, orally bioactive, BBB (blood-brain barrier) permeable (penetrable), selective H3 receptor antagonist that can inhibit [3H]histamine release with a Ki of 4.3 nM. |
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V70358 | Thonzylamine (Neohetramine) | 91-85-0 | Thonzylamine is an orally bioactive H1 histamine receptor antagonist (inhibitor) with promising antihistamine and antiallergic properties. |
|
V16855 | Triprolidine HCl | 6138-79-0 | Triprolidine HCl monohydrate is a first-generation antihistamine reagent. |
|
V70379 | VUF 5681 dihydrobromide | 639089-06-8 | VUF 5681 diHBr is a neutral antagonist of histamine H3 receptor. |
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