Ebastine

Ebastine is a histamine H1 receptor antagonist and prodrug form of carebastine (Cay-23076). Ebastine binds to histamine H1 receptors with an IC50 value of 45 nM. It is selective for histamine H1 receptors over alpha1-adrenergic and muscarinic M1 and M2 receptors (IC50s = 183, 1,100, and >10,000 nM, respectively), as well as dopamine D2 receptors and the serotonin (5-HT) receptor subtype 5-HT1A at 1 and 10 µM, respectively. Ebastine (1, 5, and 10 µM) inhibits T cell proliferation and the production of IL-4 and IL-5 in isolated human T cells. It also reduces phytohemagglutinin-induced T cell migration and decreases LPS-induced IL-6 and TNF-alpha production by macrophages isolated from peripheral blood mononuclear cells (PBMCs). Ebastine inhibits histamine-induced and allergen-induced bronchospasm in guinea pigs (ED50s = 115 and 334 µg/kg, respectively). Formulations containing ebastine have been used in the treatment of allergic rhinitis and chronic idiopathic urticaria.Formal Name: 1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone. CAS Number: 90729-43-4. Synonyms: LAS-W 090, RP 64305. Molecular Formula: C32H39NO2. Formula Weight: 469.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 2 mg/ml, Ethanol: 2 mg/ml. lambdamax: 252 nm. SMILES: O=C(C1=CC=C(C(C)(C)C)C=C1)CCCN(CC2)CCC2OC(C3=CC=CC=C3)C4=CC=CC=C4. InChi Code: InChI=1S/C32H39NO2/c1-32(2,3)28-18-16-25(17-19-28)30(34)15-10-22-33-23-20-29(21-24-33)35-31(26-11-6-4-7-12-26)27-13-8-5-9-14-27/h4-9,11-14,16-19,29,31H,10,15,20-24H2,1-3H3. InChi Key: MJJALKDDGIKVBE-UHFFFAOYSA-N.