allergic

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.

SM-324405 is an agonist of TLR7.

Experimental allergic encephalitogenic peptide (human), an EAE peptide, induces encephalomyelitis in guinea pigs [1].

Antiallergic agent-1, an Src family kinase inhibitor, is a new and valuable lead compound with potential as an anti-allergic agent.

D18024 is a phthalazinonderivat with anti-allergic and anti-histamine effect.

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.

mTOR HDAC-IN-1 (Compound 50) is a dual inhibitor of mTOR and HDAC, with IC50 values of 0.49 nM and 0.91 nM, respectively, holding potential as an anti-cancer agent [1].

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

HSR6071 is a novel orally active and potent anti-allergic agent with inhibitory effects on passive cutaneous anaphylaxis. HSR6071 showed anti-asthmatic activity in a rat model of experimental asthma.

Isoflupredone (Isoflupredonum) is a synthetic corticosteroid that acts in vivo by binding to glucocorticoid and corticosteroid receptors in animals (such as horses) to inhibit inflammatory cells and inhibit the expression of inflammatory mediators. Isoflupredone has anti-inflammatory and immunosuppressive effects and can be used to treat a variety of musculoskeletal, allergic and systemic inflammatory diseases.

Talastine is an antihistamine compound that can induce an allergic rash.

PF-03654746 is a selective antagonist of the histamine H3 receptor. PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease. PF-03654746 can be used in studies about the treatment of allergic rhinitis.

Pirodomast is a thromboxane A (TXA2) synthase inhibitor. Pirodomast inhibits leukotriene (LT) D4, C4, E4 formation and thromboxane B2 (TXB2) activity, but is weakly or ineffectively antagonistic to guinea pig bronchospasm induced by histamine, methacholine, serotonin, LTC4, or platelet-activating factor. Pirodomast is a potential antiallergic compound. Pirodomast had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is a potential antiallergic compound that inhibits the protein hydrolyzing activity of trypsin in vitro, prevents antigen-induced immediate and late asthmatic responses in allergic sheep in vivo, and inhibits antigen-induced airway hyperresponsiveness to histamine and carbachol in allergic sheep.

Eclazolast (RHC 2871) is a lipophilic anti-allergic compound that inhibits mediator release in a mast cell model.Eclazolast inhibits extracellular secretion by affecting only the direct processes associated with Fc(epsilon)RI in the cell.The effect of Eclazolast is highly dependent on the concentration of antigen that triggers the cell.

Efletirizine (UCB-28754) is a histamine receptor antagonist with inhibitory effects on the enzyme 5-lipoxygenase (5-LO), and is useful in the topical treatment of allergic diseases.

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

A-69412 (N-1-(Fur-3-ylethyl)-N-hydroxyurea) is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase. It has the potential to treat ulcerative colitis and asthma, and possibly other inflammatory and allergic conditions.

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.

lodoxamide ethyl is a new orally active anti-allergic compound for the prevention of antigen-induced bronchoconstriction and blockage of skin allergic reactions.

YM 16638 is an orally active leukotriene (LT) antagonist with triglyceride-lowering and peroxisome-increasing effects that can be used to study antigen-induced early and late airway responses in allergic sheep.

Bamaquimast (L 0042) is a proton pump inhibitor for the study of asthma-like immune system disorders and respiratory diseases.

AZD8329 is a selective and potent 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that inhibits 11β-HSD2, 17β-HSD1, 17β-HSD3, and can be used for the study of allergic reactions in humans.

JAK3-IN-7 is a potent and selective JAK3 inhibitor (IC50<0.01 μM) intended for the treatment of organ transplantation rejection, graft-versus-host reaction post-transplantation, autoimmune disorders, allergic diseases, and chronic myeloproliferative disorders.

RO0270608, the active metabolite of R411, is an orally active dual α4β1 α4β7 integrin antagonist with anti-inflammatory properties, useful for studying allergic inflammatory responses.