itching

Hydroxyzine dihydrochloride (Hydroxyzine 2HCl) is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

Hydroxyzine (Hydroxyzine free base) is an antagonist of histamine H1-receptor.

Itch-Targeting Compound 1 is an anti-itch agent effective in preventing or treating reactions from insect bites, environmental allergens, skin infections, external vermination, or itching in renal dialysis patients.

Quazolast (RHC 3988) is a potent mediator release inhibitor used as a control against ragweed antigenic nasal challenge and demonstrates superiority over placebo in preventing nasal congestion and nasal itching following such challenges.

Vapitadine is a non-sedative antihistamine compound that relieves itching caused by atopic dermatitis.

Benzyl benzoate (Benzoic acid benzyl ester) is one of the older preparations used for the therapy of scabies. Scabies is a skin infection caused by the Sarcoptes scabiei. Its symptoms are red spots, severe itching (particularly at night), and may lead to a secondary infection. Benzyl benzoate is useful in the therapy of scabies because it is lethal to this mite. It is also used for the therapy of lice affection of the body and head. Benzyl benzoate is not the therapy of choice for scabies because of its irritant properties.

Doxylamine Succinate is a pyridine derivate histamine H1 antagonist with pronounced sedative properties. Doxylamine succinate (Decapryn) competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of the gastrointestinal smooth muscle, caused by actions of histamine on bronchial and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes.

D-Panthenol (D-Pantothenyl alcohol) is an alcoholic analogue of D-pantothenic acid and cholinergic agent. D-Panthenol acts as a precursor of coenzyme A necessary for acetylation reactions and is involved in the synthesis of acetylcholine. Although the exact mechanism of the actions of D-Panthenol is unclear, it may enhance the effect of acetylcholine. D-Panthenol acts on the gastrointestinal tract and increases lower intestinal motility. It is also applied topically to the skin to relieve itching and to promote healing.

Desloratadine (Sch34117) is a long-acting piperidine derivate with selective H1 antihistaminergic and non-sedating properties. Desloratadine diminishes the typical histaminergic effects on H1-receptors in bronchial smooth muscle, capillaries and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching and spasmodic contractions of gastrointestinal smooth muscle. Desloratadine is used to provide symptomatic relieve of allergic symptoms.

Alcaftadine (Lastacaft) is an H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis.

Diflucortolone valerate (Diflucortolone 21-valerate) is a corticosteroid esterified with valeric acid. It helps to reduce itching, redness, and swelling.

Delgocitinib (JTE-052) is a JAK inhibitor and a specific JAK1/2/3/Tyk2 inhibitor (IC50=2.6-58 nM) that blocks multiple cytokine signaling pathways and inhibits pruritus, used for research on inflammatory and autoimmune diseases.

MRGPRX2 modulator-3 (Compound 4-400) is a quinoline derivative and an MRGPRX2 regulator. It is utilized in the investigation of MRGPRX2-related conditions, including allergies, itching, pain, inflammation, and autoimmune diseases.

MRGPRX4 modulator-3 (Compound 1C) is an allosteric negative modulator of MAS-related G-protein coupled receptor X4 (MRGPRX4). It significantly inhibits the activation response induced by Nateglinide (an orthosteric agonist), with an IC50 of 337 nM. MRGPRX4 modulator-3 is applicable in studies related to chronic itching, particularly cholestatic pruritus, and pain.

Trpvicin is a potent and subtype-selective TRPV3 inhibitor, exhibiting IC50 values of 0.41 μM for hTRPV3-WT and 0.22 μM for hTRPV3-G573S mutants. It shows only weak inhibitory effects on other TRP family members (such as TRPV1/2/4/5/6, TRPA1, and TRPM8). By binding to the VSLD-PD site, Trpvicin stabilizes the closed state of TRPV3 channels, and in the G573S mutant, it enters the central cavity, enhancing inhibition through symmetry restructuring and pore blockage. In mouse models, Trpvicin can inhibit itching and hair loss and is applicable for research related to inflammation and immunology.

Olopatadine is an orally active, selective histamine H1 receptor antagonist and mast cell stabilizer. It inhibits the release of immunostimulatory pro-inflammatory mediators from human conjunctival mast cells and can be used in research on allergic conjunctivitis.

Isothipendyl is the first generation of H1 antagonists (antihistamines) and anticholinergics and has an effect on itching.

Methdilazine Hydrochloride (Bristaline) is a histamine H1 receptor antagonist used in the treatment of dermatologic conditions and for the relief of itching caused by allergies or rhinitis.

Phenindamine Tartrate is an antihistamine and anticholinergic drug closely related to cyproheptadine. It is used to treat symptoms of the common cold and allergies, such as sneezing, itching, rashes, and hives.

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

Kallikrein 5-IN-2 is a potent inhibitor of Kallikrein KLK5, exhibiting selectivity with a pIC50 value of 7.1. By inhibiting KLK5, it has the potential to normalize epidermal shedding, thereby reducing associated inflammation and itching.

γ-Isofagarine (Iso-γ-fagarine), an alkaloid extractable from the root bark of Dictamnus angustifolius, has applications in the research of various conditions including rheumatism, bleeding, itching, jaundice, chronic hepatitis, and skin diseases [1].

EP3 antagonist 7 (Compound II), an EP3 receptor antagonist, is applicable in researching conditions such as itching, pain, dysuria, or stress disorders [1].

Fluocinolone, a corticosteroid, is used to alleviate redness, itching, swelling, and other discomforts caused by skin conditions [1].