histamine release

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

Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

Nesosteine Lithium is a novel mucoregulatory that inhibits Herxheimer microconvulsions in guinea pigs and inhibits ovalbumin-induced histamine release from sensitized trachea.Nesosteine Lithium protects against ovalbumin-induced bronchospasm but is ineffective against histamine- and acetylcholine-induced bronchospasm. Nesosteine Lithium protected against ovalbumin-induced bronchospasm but not histamine- and acetylcholine-induced bronchospasm.

Mebhydrolin napadisylate (Incidal) is an antihistamine used to relieve allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis.

Nylidrin hydrochloride (Buphenine HCl) was an effective inhibitor of the IgG1-mediated release of histamine from passively sensitized guinea pig lung slices, and of the IgE-mediated release of histamine from passively sensitized rat peritoneal mast cells and human basophils.

Ethylparaben (Ethyl parahydroxybenzoate) is a Standardized Chemical Allergen. The physiologic effect of ethylparaben is by means of Increased Histamine Release, and Cell-mediated Immunity.

Chlorquinaldol (5,7-Dichloro-8-hydroxy-2-methylquinoline) is a Standardized Chemical Allergen. The physiologic effect of chlorquinaldol is by means of Increased Histamine Release, and Cell-mediated Immunity.

Butylparaben (Butyl 4-hydroxybenzoate) is a standardized chemical allergen, increasing histamine release, and cell-mediated immunity.

Ketotifen fumarate (HC 20511 fumarate) is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.

Eugenol (Allylguaiacol) is a Standardized Chemical Allergen. The physiologic effect of eugenol is by means of Increased Histamine Release and Cell-mediated Immunity.

Alginic acid (Snow acid algin G) is a natural polysaccharide extracted from brown seaweeds with anti-anaphylactic and anti-inflammatory activities. Alginic acid inhibits histamine release and can be used in the food industry.

The physiologic effect of Methyl Paraben (Nipagin) is by means of Increased Histamine Release, and Cell-mediated Immunity. Methyl Paraben (Nipagin) is an antimicrobial agent, preservative, flavouring agent. Methyl Paraben (Nipagin) is a constituent of cloudberry, yellow passion fruit, white wine, botrytised wine and Bourbon vanilla.The physiologic effect of Methyl Paraben (Nipagin) has been shown to exhibit anti-microbial function.

Chlorphenesin (Chlorophenesin) is an antigen-associated immunosuppressant that inhibits IgE-mediated histamine release. It is also used as an antimycotic agent.

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

Epinastine (WAL801), a potent, selective, and orally-active antihistamine and mast cell stabilizer, functions as a histamine H1 receptor antagonist. It also inhibits IL-8 release from human eosinophils, showcasing antiallergic action [1] [2] [3] [4].

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg kg and prevents memory deficits induced by the AMPA kainate glutamate receptor antagonist NBQX at 0.1 mg kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

CI-949 is an allergic mediator release inhibitor that inhibits the release of leukotriene C4 D4 (LTC4 LTD4), histamine, and thromboxane B2 (TXB2) with IC50 values of 0.5 μM, 11.4 μM, and 0.1 μM, respectively.

Quinotolast sodium inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner in the concentration range of 1-100 μg mL.

Tazanolast, a selective mast-cell-stabilizing drug, inhibits the release of chemical mediators (histamine and leukotrienes) from mast cells, reduces inflammation, and is used in the treatment of allergic disorders, such as asthma and allergic rhinitis.

GSK 189254A is a histamine H3 receptor antagonist for the treatment of narcolepsy. Histamine H3 receptor antagonists have been shown to increase the release of neurotransmitters in the brain and to enhance cognition in vivo. The compound may also be usefu

Clobenpropit 2HBr is a histamine H3 receptor antagonist. It has neuroprotective effects via stimulation of GABA release in the brain.

8 Hydroxy PIPAT oxalate is a selective 5-HT1A receptor agonist that enhances the spontaneous release of histamine by promoting the degranulation of mast cells in guinea pig and human intestinal preparations. By activating the serotonin signaling pathway, this compound demonstrates potential in regulating gastrointestinal functions and offers insight into the management and suppression of functional gastrointestinal disorders such as irritable bowel syndrome. Its effects in increasing histamine release could play a crucial role in gastrointestinal regulation.

Tixanox sodium effectively blocks histamine release in the lungs triggered by anti-IgE. It has also been demonstrated that when administered orally, Tixanox sodium can successfully counteract exercise-induced asthma.