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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V86642 | (±)-Carbinoxamine | 486-16-8 | (±)-Carbinoxamine is a histamine H1 receptor antagonist. |
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V4406 | ABT-239 | 460746-46-7 | ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist/inverse agonist developed by Abbott with stimulant and nootropic effects, and has been investigated as a treatment for ADHD, Alzheimer's disease, and schizophrenia. |
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V89035 | Anticancer agent 192 | Anticancer agent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist that has no affinity for muscarinic and hERG. | |
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V4935 | Astemizole | 68844-77-9 | Astemizole (formerly R-43512; Hismanal) is a novel, potent and second-generation antihistamine drug with a long duration of action and is used to diminish allergic symptomsby acting as ahistamine H1-receptor antagonist (IC50= 4 nM). |
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V1238 | Azatadine dimaleate | 3978-86-7 | Azatadine dimaleate (SCH10649; SCH-10649; Idulamine; Idulian; Lergocil; Optimine; Zadine), the dimaleate salt of azatadine,is a potent histamine and cholinergic inhibitor that has beenapproved for treating allergic rhinitis and chronic urticaria. |
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V1209 | Azelastine HCl (Allergodil) | 79307-93-0 | Azelastine HCl(Allergodil; Astelin; Optivar; Rhinolast; Azeptin),the hydrochloride salt of azelastine, is a potent, 2nd-generation, and selective histamine receptor antagonist used for the treatment of rhinitis. |
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V4516 | Bavisant dihydrochloride hydrate | 1103522-80-0 | Bavisant dihydrochloride hydrate (also known as JNJ-31001074 dihydrochloride hydrate) is a novel, highly selective, orally bioactive antagonist of the human H3 receptor with a novel mechanism of action which involves wakefulness and cognition. |
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V8638 | Bepotastine | 125602-71-3 | Bepotastine (also known as TAU 284; Bepreve) is a second generation, non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
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V1212 | Bepotastine Besilate (Bepreve) | 190786-44-8 | Bepotastinebesilate(bepotastine besylate; TAU-284; TAU284;Bepreve; Talion), the besylate salt ofBepotastine, is a 2nd generation, non-sedating, and selective antagonist of histamine 1 (H1) receptor with a pIC50 of 5.7. |
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V1236 | Betahistine 2HCl | 5579-84-0 | Betahistine dihydrochloride (formerly PT 9; PT9; trade names Veserc, Serc, Hiserk, Betaserc, Vergo), the dihydrochloride salt of Betahistine which was pproved in EU in 1970s for treating Ménière's disease, is a potent antagonist of histamine H3 receptor used as an anti-vertigo drug. |
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V12560 | Betahistine mesylate | 54856-23-4 | Betahistine mesylate (also known as PT-9), the mono-HCl salt of Betahistine, is a potent histamine H3 receptor inhibitor with IC50 of 1.9 μM. |
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V90046 | Bisfentidine | 96153-56-9 | Bisfentidine is an H2 receptor antagonist. |
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V86638 | BMY-25368 hydrochloride | 86134-36-3 | BMY-25368 hydrochloride is a histamine H2 receptor antagonist and can be used as a gastric acid secretion inhibitor. |
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V4908 | Bromodiphenhydramine HCl | 1808-12-4 | Bromodiphenhydramine (Bromazine; trade names: Ambodryl, Ambrodil and others) hydrochloride is the hydrochloride salt form of bromodiphenhydramine, a synthetic ethanolamine with histamine H1 antagonistic and sedative properties. |
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V1231 | Brompheniramine maleate | 980-71-2 | Brompheniramine (Bromfed, Dimetapp, Bromfenex, Dimetane, BPN, Lodrane), the maleate salt of Brompheniramine which is an OTC drug for cold and allergic rhinitis, is a first-generation antagonist of the histamine H1 receptors. |
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V1226 | Buclizine HCl (UCB-4445) | 129-74-8 | Buclizine hydrochloride (AH-2526, UCB 4445; AH2526; UCB-4445, Buclina, Longifene, Posdel, Vibazine), the hydrochloride salt of buclizine which is used for motion sickness, is a piperazine derivative and a sedating antihistamine with antimuscarinic and moderate sedative action. |
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V1218 | Cetirizine DiHCl (P071) | 83881-52-1 | Cetirizine 2HCl (P-071; UCB P071; Reactine; Zyrtec; Alerlisin; AC-170; P071),the dihydrochloride salt of cetirizine and a major active metabolite of hydroxyzine, isa 2nd-generation antihistamine used in the treatment of allergies, hay fever, angioedema, and urticarial etc. |
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V6698 | Chloropyramine | 59-32-5 | Chloropyramine hydrochloride (Alergosan, Nilfan, Sinopen, Allergan hydrochloride, Suprastin) is an antihistamine drug acting as a histamine receptor H1 antagonist. |
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V29900 | Chloropyramine hydrochloride | 6170-42-9 | Chloropyramine hydrochloride (Alergosan, Allergan hydrochloride, Nilfan, Sinopen, Suprastin), the hydrochloride salt of Chloropyramine, is a potentantihistamine drug acting as a histamine receptor H1 antagonist. |
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V1240 | Chlorpheniramine Maleate | 113-92-8 | Chlorpheniramine Maleate (Piriton; Chlortrimeton; Deconamine; Neorestamin; NCIC-55265; NCIC55265; Chlo-Amine; Chlor-100; Chlor-Trimeton), the Maleate salt of Chlorpheniramine, is a potent and 1st-generation alkylamine-based histamine H1 receptor antagonist with anti-allergic effects. |
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