| 货号 | 11999-10mg |
| 描述 | Olopatadine is a potent, selective antagonist of the H1 histamine receptor (Ki = 16-41.1 nM), with much lower affinities for the H2 and H3 receptors (Ki = 43.4 and 172 μM, respectively).1,2 It blocks histamine-induced phosphoinositide turnover in isolated cells (IC50 = 9.5-39.9 nM) and prevents passive cutaneous anaphylaxis in rats (ED50 = 49 μg/kg) and anaphylactic bronchoconstriction in guinea pigs (ID50 = 30 μg/kg).1,2 Olopatadine is effective in treating allergic rhinitis and conjunctivitis.3,4,5 It also suppresses itch in patients with well-controlled chronic urticaria.6 In humans, this antihistamine does not cause cognitive or psychomotor impairment at therapeutic doses.7 |
| 别名 | Allerock;ALO 4943A;KW 4679;Olopine;Patanase; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ohshima, E.,Otaki, S.,Sato, H., et al. Synthesis and antiallergic activity of 11-(aminoalkylidene)-6,11-dihydrodibenz[b,e]oxepin derivatives. Journal of Medicinal Chemistry 35(11), 2074-2084 (1992). 2.Sharif, N.A.,Xu, S.X., and Yanni, J.M. Olopatadine (AL-4943A): Ligand binding and functional studies on a novel, long acting H1-selective histamine antagonist and anti-allergic agent for use in allergic conjunctivitis. Journal of Ocular Pharmacology and Therapeutics 12(4), 401-407 (1996). 3.Kaise, T.,Ohmori, K.,Sakakura, Y., et al. The effect of KW-4679, an antiallergic drug, on experimental allergic rhinitis in guinea pigs: Effects on nasal blockage. Japanese Journal of Pharmacology 69, 435-438 (1995). 4.Yanni, J.M.,Stephens, D.J.,Miller, S.T., et al. The in vitro and in vivo ocular pharmacology of olopatadine (AL-4943A), an effective anti-allergic/antihistaminic agent. Journal of Ocular Pharmacology and Therapeutics 12(4), 389-400 (1996). 5.Maiti, R.,Jaida, J.,Rahman, J., et al. Olopatadine hydrochloride and rupatadine fumarate in seasonal allergic rhinitis: A comparative study of efficacy and safety. J.Pharmacol.Pharmacother. 2(4), 270-276 (2011). 6.Makino, T.,Takegami, Y.,Rehman, M.U., et al. Maintenance of remission with low-dose olopatadine hydrochloride for itch in well-controlled chronic urticaria. Clin.Cosmet.Investig.Dermatol. 5, 141-146 (2012). 7.Kamei, H.,Isaji, A.,Noda, Y., et al. Effects of single therapeutic doses of promethazine, fexofenadine and olopatadine on psychomotor function and histamine-induced wheal- and flare-responses: A randomized double-blind, placebo-controlled study in healthy volunteers. Archives of Dermatological Research 304, 263-272 (2012). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 373.9 |
| 分子式 | C21H23NO3 • HCl |
| CAS号 | 140462-76-6 |
| 稳定性 | ≥ 2 years |
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