antipruritic

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived relaxing factor, nitric oxide.

Crotamiton (Eurax) is an antipruritic and a scabicidal agent available as a lotion or cream for topical use only. It is a colorless to slightly yellowish oil with a faint amine-like odor. It is miscible with methanol and with alcohol.

Pramocaine hydrochloride (Pramoxine HCl), a topical anesthetic, is served as an antipruritic.

Tetracaine hydrochloride (Amethocalne HCl) (Pontocaine), a potent local anaesthetic, is a channel function allosteric inhibitor. It is primarily used as an antipruritic and topically in ophthalmology, and it has been used for surface and spinal anesthesia.

Clobetasol propionate (CGP9555) exerts its effect by binding to cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor-mediated gene expression. This results in the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Clobetasol Propionate is the propionate salt form of clobetasol, a topical synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. Specifically, clobetasol propionate appears to induce phospholipase A2 inhibitory proteins, thereby controlling the release of the inflammatory precursor arachidonic acid from membrane phospholipids by phospholipase A2.

Camphor (2-Camphanone) is a bicyclic monoterpene ketone found widely in plants, especially CINNAMOMUM CAMPHORA. It is used topically as a skin antipruritic and as an anti-infective agent.

Flumethasone (RS-2177) is a glucocorticoid receptor agonist, with anti-inflammatory, antipruritic and vasoconstrictive properties.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

Alimemazine hemitartrate (Trimeprazine hemitartrate) is aphenothiazine derivative that is used as an antipruritic. It also acts as a sedative, hypnotic, and antiemetic for prevention of motion sickness.

Hydrocortisone Valerate (Westcort) has anti-inflammatory, antipruritic and vasoconstrictive properties.

Thonzylamine hydrochloride (Resistab) is an anticholinergic and antihistamine used as an antipruritic.

Prednicarbate (Hoe 777) is a Corticosteroid Hormone Receptor Agonist. Prednicarbate has antipruritic, anti-inflammatory, and vasoconstrictive properties. It also decreases the number of circulating lymphocytes by inhibiting the production of vasodilators such as nitric oxide and prostacyclin.

Hydrocortisone 17-butyrate (Cortisol 17-butyrate) is a synthetic glucocorticoid receptor agonist with antiinflammatory, antipruritic and vasoconstrictive effects.

Alimemazine (Trimeprazine) is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist. Alimemazine also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs.

JNJ-39758979 is a selective and high-affinity histamine H4 receptor antagonist (Kis: 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively). JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2

Flumethasone pivalate (Locorten) has antipruritic, anti-inflammatory, and vasoconstrictive properties and can be used in studies about adrenocortical suppression, cutaneous atrophy, plasma transcortin binding, and telangiectasia.

Alclometasone dipropionate (Sch 22219) is a synthetic glucocorticoid, a steroidal compound with antiproliferative, anti-inflammatory, anti-allergic, antipruritic, and vasoconstrictive properties, which is used in the study of skin inflammation.

DA 5018 is a capsaicin derivative and is also a new non-narcotic analgesic. It has an antipruritic effect.

A-943931 is a histamine H4receptor antagonist (Ki= 3.8 nM).1In vivo, A-943931 inhibits scratching induced by clobenpropit in mice (ED50= 26 μmoles/kg, i.p.). 1.Milicic, I., Witte, D.G., Miller, T.L., et al.Identification of two potent and selective histamine H4 receptor antagonists with antipruritic activityFASEB J.23(S1)760.768-760.768(2009)

INCB38579 is a selective, orally active, histamine H4 receptor (HH4R) antagonist that crosses the blood-brain barrier and acts on hH4R (IC50: 4.8 nM), mH4R (IC50: 42 nM), and rH4R (IC50: 32 nM). INCB38579 has anti-inflammatory and antipruritic effects.

Halobetasol propionate (BMY-30056) is the propionate salt form of halobetasol, a synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictor activities. Halobetasol, a topical steroid, diffuses across cell membranes to interact with cytoplasmic corticosteroid receptors located in both the dermal and intradermal cells, thereby activating gene expression of anti-inflammatory proteins mediated via corticosteroid receptor response element. Specifically, this agent induces phospholipase A2 inhibitory proteins, which inhibit the release of arachidonic acid, thereby inhibiting the biosynthesis of potent mediators of inflammation, such as prostaglandins and leukotrienes. As a result, halobetasol reduces edema, erythema, and pruritus through its cutaneous effects on vascular dilation and permeability.

Thenalidine is an antihistamine with anticholinergic properties used as an antipruritic drug. It was withdrawn from the US, Canadian, and UK markets due to a risk of neutropenia. Thenalidine is an antagonist of the H1-receptor.

Chlorphenoxamine (Contristamine) is an antihistamine and anticholinergic utilized as an antipruritic and antiparkinsonian agent.

MOR agonist-4 (2d), having an EC50 of 11 nM, is a G protein-biased agonist of the Kappa opioid receptor (KOR). This compound features a triazole-based, electron-withdrawing CF3 group and a bias factor of 38. MOR agonist-4 is utilized for antipruritic and analgesic applications.