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 |
|---|---|---|---|---|
|
V79880 | Pheniramine-d6 maleate (Prophenpyridamine-d6 (maleate); Tripoton-d6 (maleate)) | Pheniramine-d6 (maleate) is the deuterium labelled form of Pheniramine maleate. | |
|
V85428 | Pirdonium bromide | 35620-67-8 | |
|
V107910 | Promethazine sulfoxide | 7640-51-9 | Promethazine sulfoxide is a metabolite of the histamine H1 receptor antagonist promethazine, which is formed from promethazine via the cytochrome P450 (CYP) isozyme CYP2D6. |
|
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. |
|
V85156 | Spinacetin | 3153-83-1 | |
|
V4572 | SUN-1334H | 607736-84-5 | SUN 1334H is a novel, potent, orally bioactive, and highly selectiveH1 receptorantagonist withKiof 9.7 nM. |
|
V99495 | TAAR1 agonist 2 | 1804128-38-8 | TAAR1 agonist 2 (compound 30) is a full agonist (pEC50=7.5) of trace amine-associated receptor 1 (TAAR1). |
|
V89036 | Talastine | 16188-61-7 | Talastine is a potent H1-antihistamine. |
|
V94428 | Talastine hydrochloride | 16188-76-4 | Tastatin hydrochloride is an antihistamine with anti-allergic effects. |
|
V104230 | UR-AK49 | 902154-32-9 | UR-AK49 (Compound 11) is a human histamine H1 and H2 receptor agonist. |
|
V93657 | Vapitadine | 793655-64-8 | Valadin is a nonsedating antihistamine that relieves itching associated with atopic dermatitis. |
|
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. |
|
V86641 | Zaltidine dihydrochloride | 90274-23-0 | Zaltidine (CP-5736) dihydrochloride is a highly specific H2 receptor antagonist with antisecretory activity. |
|
V3402 | Ibipinabant racemate | 362519-49-1 | Ibipinabant (racemic), also known as (±)-SLV319; BMS-646256; JD-5001, is the racemic mixture of SLV319 and is a novel, potent and selective antagonist/inverse agonist of cannabinoid-1 (CB-1) receptor with an IC50 of 22 nM. |
|
V29268 | Epinastine (WAL801) | 80012-43-7 | Epinastine (also known as WAL-801CL HCl) is a potent antihistamine H1 without sedative activity and a mast cell stabilizer that is used in eye drops for the treatment of allergic conjunctivitis. |
|
V3731 | Emedastine | 87233-61-2 | Emedastine is a novel, potent, high affinity, selective, second generation H1-receptor antagonist with pre-clinically well-documented anti-allergic effects. |
|
V3412 | Clemizole | 442-52-4 | Clemizole (also known as AL 20, P 48, and/or Reactrol), is a potent inhibitor of transient receptor potential channel TRPC5 (Canonical transient receptor potential channel 5) and also an H1 histamine receptor antagonist. |
|
V1215 | Lidocaine (Lignocaine) | 137-58-6 | Lidocaine (Alphacaine; NSC-40030; NSC40030; Lignocaine),a local anesthetic and cardiac depressant used as an antiarrhythmia agent,is a potent and selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. |
|
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. |
|
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. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
