Histamine Receptor

Pitolisant hydrochloride (Ciproxidine) is a potent and selective inverse agonist of the histamine H3 receptor(Ki : 0.16 nM).

(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.

Rocastine (AHR-11325) is a selective and potent non-sedating H1 receptor antagonist.

Bamirastine inhibits ligand binding to recombinant human histamine H1 receptor (rhH1R) with an IC50 of 17.3 nM and possesses an inhibitory effect on allergic skin inflammation.

Lavoltidine (Loxtidine) is a potent and selective H2 receptor antagonist, orally active and irreversible, that inhibits gastric acid secretion and is used in the treatment of gastroesophageal reflux disease.

Sodium butanoate (Sodium Butyrate) is the sodium salt of butyrate with potential antineoplastic activity. Butyrate, a short chain fatty acid, competitively binds to the zinc sites of class I and II histone deacetylases (HDACs).

ReN-1869 is a novel selective histamine H(1) receptor antagonist with anti-neurogenic pain and anti-inflammatory activity for the study of neurological diseases.

Escitalopram (Seroplex) is a furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.

Nepetin (6-Methoxyluteolin) has antioxidant activity, it is a potent inhibitor of histamine release and calcium influx via down-regulation of the FcεRI α chain.

GSK-239512 is an antagonist of H3 receptor and can be used in studies about the treatment of cognitive dysfunction in neurodegenerative disorders.

Clemizole, an H1 histamine receptor antagonist, inhibits NS4B's RNA binding and hepatitis C virus (HCV) replication.

Meclizine dihydrochloride (NSC28728) is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.

Vapitadine dihydrochloride(R-129160 2HCl) is a novel, potent, selective and non-sedating compound with inhibitory effects on histamine H1.

Carebastine, the active metabolite of Ebastine, is an antagonist of the histamine H1 receptor.

Adriforant (PF-3893787,ZPL-3893797) is a competitive H4 (histamine receptor 4) antagonist that antagonizes histamine-induced phosphorylation of ERK, normalizes histamine-induced transcriptional changes in mast cells and reduces histamine-dependent Ca2+ fluxes in neurons, which alleviates itching and skin inflammation in mice

Proxyfan (Proxifan) is a high-affinity protean antagonist agonist of histamine H3 receptors with a full spectrum of pharmacological activity ranging from full agonist to full inverse agonist(antagonist), depending on the competition between constitutively active and resting H3 receptors within a given tissue or brain region.Proxyfan acts as a neutral antagonist in the feeding-associated ventral medial nucleus of the hypothalamus, and as a agonist in the basolateral amygdala of the rat (BLA).

AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.

ICI 162,846 is an orally active and potent H2 receptor antagonist that inhibits gastric secretion and may be used in the study of duodenal ulcers.

PF-03654764 is an orally active, potent, and selective histamine H3 receptor antagonist with Ki values of 1.2 nM for human H3 and 7.9 nM for rat H3. It is often co-administered with Fexofenadine for the treatment of allergic rhinitis.

Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties. Amitriptyline is widely used to treat depression and neuropathic pain.

Lodoxamide (Lodoxamidum) is an antiallergic drug acting as a mast-cell stabilizer. It is effective in the treatment of asthma and allergic conjunctivitis.

KP136 (AL136) is an orally active anti-allergic compound that inhibits histamine release and is used in studies of asthma and allergic edema.

DF-1111301 is a novel anti-allergic compound with anti-histamine H1 and anti-PAF activity.

JNJ-39220675 (JNJ 39220675) is a selective and brain permeable histamine H3 receptor antagonist.