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 |
|---|---|---|---|---|
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V1210 | Mianserin HCl (ORG GB-94 HCl) | 21535-47-7 | Mianserin HCl (formerly ORG GB-94; ORG-GB 94; Depnon, Lantanon, Lerivon, Lumin, Norval, Tolvon), the hydrochloride salt of mianserin which is a psychoactive tetracyclic compound, is a novel and potent antagonist (inverse agonist) of H1 histamine receptor and 5-HT serotonin receptors used for the treatment of depression. |
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V1234 | Mizolastine (SL 850324) | 108612-45-9 | Mizolastine (Mizollen; SL 85.0324; Mistalin; SL-850324;SL 850324; Mistamine; Mizolastina) is a histamine H1-receptor antagonist with anti-allergic effects. |
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V29682 | N-Acetylhistamine | 673-49-4 | N-Acetylhistamine is a histamine metabolite. |
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V1219 | Nizatidine | 76963-41-2 | Nizatidine (Tazac, Axid, LY-139037, LY 139037, LY139037) is a potent histamine H2 receptor antagonist used in the treatment of peptic ulcer disease and gastroesophageal reflux disease. |
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V26713 | NSC19005 | 5452-87-9 | NSC19005 (Betahistine EP Impurity C) is an impurity of Betahistine and is structurally related to Betahistine. |
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V1222 | Olopatadine HCl (ALO4943A; KW4679) | 140462-76-6 | Olopatadine HCl (Pataday; Patanase; KW-4679; ALO-4943A; ALO4943A; KW4679), the hydrochloride salt of olopatadine, is a 2nd-generation, selective histamine H1 receptor (IC50 of 559 μM for the release of histamine) antagonist and also a mast cell stabilizer used to treat itching associated with allergic conjunctivitis (eye allergies), it may also be used for the treatment of steroid rebound (red skin syndrome). |
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V1989 | Osthole | 484-12-8 | Osthol (Osthol; Ostol; NSC 31868) is an O-methylated coumarin analog and a natural product which is found in the plants such as Cnidium monnieri, Angelica archangelica and Angelica pubescens. |
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V1241 | Pemirolast potassium (TWT-8152; BMY 26517) | 100299-08-9 | Pemirolast potassium (formerly TWT 8152; BMY 26517; TWT-8152; BMY-26517; Alegysal and Alamast), the potassium salt of Pemirolast, is a poten and orally bioactive histamine H1 antagonist and mast cell stabilizer with potential antiallergic effects. |
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V79880 | Pheniramine-d6 maleate (Prophenpyridamine-d6 (maleate); Tripoton-d6 (maleate)) | Pheniramine-d6 (maleate) is the deuterium labelled form of Pheniramine maleate. | |
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V4307 | PITOLISANT | 362665-56-3 | Pitolisant (formerly BF2.649; Tiprolisant; BF2649; Ciproxidine; Wakix) is a novel, potent and selective nonimidazole inverse agonist of the recombinant human histamine H3 receptor with Ki of 0.16 nM. |
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V12519 | Psoralenoside | 905954-17-8 | Psoralenoside is a benzofuran glycoside developed from Psoralea corylifolia. |
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V1211 | Ranitidine HCl | 66357-59-3 | Ranitidine HCl (ZANTAC; AH-19065; AH 19065; Tanidina; Toriol; Fendibina; Gastridina; Sostril; Zantic; Ranisen), the hydrochloride salt of Ranitidine, is a histamine H2-receptor antagonist with an IC50 of 3.3 ± 1.4 uM. |
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V1229 | Roxatidine acetate HCl (HOE 760) | 93793-83-0 | Roxatidine Acetate HCl (HOE-760; TZU0460; HOE760; TZU-0460; Gastralgin; Altat; Roxit), the hydrochloride salt of Roxatidine Acetate, is a specific and competitive histamin H2-receptor antagonist with antiulcer activity. |
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V2041 | Rupatadine | 158876-82-5 | Rupatadine (also known as UR-12592) is a potent inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively. |
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V1245 | Rupatadine Fumarate (UR-12592) | 182349-12-8 | Rupatadine Fumarate (UR-12592; UR12592; Pafinur; Rupax; Rupafin; Alergoliber; Rinialer; Ralif), the fumarate salt of Rupatadine, is a potent inhibitor of PAFR and antagonist of histamine (H1) receptor used to treat allergies. |
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V2789 | S 38093 | 862896-30-8 | S 38093 is a novel brain-penetrant antagonist (inverse agonist) of the H3 (histamine H3) receptor with Kiof 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively. |
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V4572 | SUN-1334H | 607736-84-5 | SUN 1334H is a novel, potent, orally bioactive, and highly selectiveH1 receptorantagonist withKiof 9.7 nM. |
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V1232 | Tetrandrine (NSC-77037) | 518-34-3 | Tetrandrine (also called Fanchinine; Sinomenine A; d-tetrandrine; formerly NSC-77037), a bis-benzylisoquinoline alkaloid derived from Stephania tetrandra, is a novel and potent calcium channel blocker which inhibits voltage-gated Ca2+ current (ICa) and Ca2+-activated K+ current. |
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V1237 | Tripelennamine HCl | 154-69-8 | Tripelennamine HCl (Pyrinamine; Stanzamine; Tripelennamine; Pyribenzamine), the hydrochloride salt of Tripelennamine, is a potent histamine H1 receptor antagonist that has been widely used as an antipruritic agent. |
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V3236 | VUF10460 | 1028327-66-3 | VUF10460 is a non-imidazole agonist of the histamine H4 receptor which binds to rat H4 receptor with a pKi of 7.46. |
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