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 |
|---|---|---|---|---|
|
V2939 | GSK189254A | 720690-73-3 | GSK189254A (also known as GSK189254) is a novel histamine H(3) receptor antagonist with high affinity for human (pK(i) = 9.59 -9.90) and rat (pK(i) = 8.51-9.17) H(3) receptors. |
|
V30332 | Histamine | 51-45-6 | Histamine is an organic nitrogen compound and endogenous hormone involved in local immune responses, as well as regulating physiological functions in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. |
|
V1224 | Histamine 2HCl (Ergamine) | 56-92-8 | Histamine 2HCl(Ergamine),the dihydrochloride salt of histamine, is an organic nitrogen compound and an endogenous metabolite involved in local immune responses, as well as regulating physiological function in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. |
|
V1227 | Histamine Phosphate | 51-74-1 | Histamine (phosphate) is a strong histamine receptor agonist/activator and vasodilator neuroagent, capable of activating nitric oxide synthase. |
|
V22353 | Hydroxyzine | 68-88-2 | Hydroxyzine is a potent histamine H1-receptor antagonist which inhibits the binding of [3H]pyrilamine/[3H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM. |
|
V1243 | Hydroxyzine 2HCl | 2192-20-3 | Hydroxyzine 2HCl (NSC-169188; NSC169188; Arcanax; Neurolax; Orgatrax; Pamoate, Hydroxyzine; Vistaril),the dihydrochloride salt of hydroxyzine, is a potent histamine H1-receptor antagonist and an antihistamine drug used in the treatment of itchiness, anxiety, and nausea. |
|
V80340 | Hydroxyzine-d4 dihydrochloride (hydroxyzine D4 hydrochloride) | Hydroxyzine-d4 (di-HCl) is the deuterated form of Hydroxyzine. | |
|
V3402 | Ibipinabant | 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. |
|
V4515 | JNJ-31001074 | 929622-08-2 | Bavisant (also known as JNJ-31001074) is a novel, highly selective, orally bioactive antagonist of the human H3 receptor with a novel mechanism of action which involves wakefulness and cognition. |
|
V4499 | JNJ-39758979 | 1046447-90-8 | JNJ-39758979 is a novel, potent and selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM. |
|
V1239 | JNJ-7777120 | 459168-41-3 | JNJ-7777120 (JNJ7777120; JNJ 7777120), an indole analog, is a potent and selective non-imidazole-based histamine H4R receptor antagonist that can reduce allergic and asthmatic symptoms. |
|
V1233 | Ketotifen Fumarate (HC 20511) | 34580-14-8 | Ketotifen Fumarate (HC20511; Ketotifene, Zaditor, Zaditen, Ketotiphen), the fumaric acid salt of ketotifen, is a second-generation and noncompetitive H1-antihistamine and mast cell stabilizer used to treat allergic symptoms and to prevent asthma attacks. |
|
V1235 | Lafutidine (FRG-8813) | 118288-08-7 | Lafutidine (formerly FRG-8813; FRG8813; trade name: Protecadin; Stogar) is a 2nd-generationhistamine H2 receptor antagonist used to treat gastric ulcers, duodenal ulcers, and wounds in the stomach associated with chronic gastritis. |
|
V1225 | Levodropropizine (DF-526) | 99291-25-5 | Levodropropizine [(S)-(-)-Dropropizine; DF 526; DF-526; DF526; Levotuss], the S-isomer of dropropizine, is a histamine receptor inhibitor used as a cough suppressant. |
|
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. |
|
V37611 | LML134 | 1542135-76-1 | LML134 is a novel, orally bioactive and highly selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. |
|
V24200 | Lodoxamide (U42585E) | 53882-12-5 | Lodoxamide(U-42585E; Alomide) is an antiallergic agent acting as a mast cell stabilizer, as well as a potent agonist of GPR35 with an EC50 of 1.61 nM in a β-arrestin-2 interaction assay using CHO-K1 cells expressing the human receptor. |
|
V24325 | Lodoxamide Tromethamide | 63610-09-3 | Lodoxamide Tromethamide (U-42585E), theTromethamide salt of Lodoxamide, isan antiallergic drug acting asa potent GPR35 agonist with an EC50 of 1.61 nM in a β-arrestin-2 interaction assay using CHO-K1 cells expressing the human receptor. |
|
V1208 | Loratadine (Loratidine; SCH 29851) | 79794-75-5 | Loratadine (formerly SCH29851; SCH-29851; Claritin; Loratidine; Clarityn; Alavert) is a potent and 2nd-generation histamine H1 receptor antagonist which has been approved for the treatment ofallergies such as allergic rhinitis and urticaria. |
|
V1216 | Meclizine 2HCl | 1104-22-9 | Meclizine 2HCl (Ru Vert M; Ru-Vert-M; RuVertM; NSC28728; NSC-28728), the dihydrochloride salt of meclizine, is a potent histamine H1 receptor antagonist used to treat nausea and motion sickness, and has anti-histamine, anti-muscarinic and anti-oxidative phosphorylation properties. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
