产品说明书

Mizolastine

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Chemical Structure| 108612-45-9 同义名 : 咪唑司汀 ;SL 850324
CAS号 : 108612-45-9
货号 : A300693
分子式 : C24H25FN6O
纯度 : 98%
分子量 : 432.493
MDL号 : MFCD00864625
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(57.8 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • H1 receptor

    Histamine H1 receptor, IC50:47 nM
描述 Mizolastine, a second generation antihistamine agent, a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors. Mizolastine 10 mg/day is generally well tolerated, with the most common adverse events being drowsiness (7%), fatigue (2%), increased appetite (2%) and dry mouth (2%)[3]. Mizolastine is effective and well tolerated in the long-term treatment of perennial allergic rhinoconjunctivitis[4]. Mizolastine blocked HERG1 K(+) channels expressed in Xenopus oocytes with an estimated IC50 of 3.4 mM. In HEK 293 cells stably transfected with HERG1 cDNA, extracellular application of mizolastine exerted a dose-related inhibitory action on I(HERG1), with an IC50 of 350+/-76 nM. Furthermore, mizolastine dose-dependently inhibited HERG1 K(+) channels constitutively expressed in SH-SY5Y human neuroblastoma clonal cells[5]. Good activity of both cetirizine 10 mg and mizolastine 10 mg in inhibiting skin wheal and flare reactions to histamine[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01928316 Healthy Phase 1 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL
参考文献

[1]Lorette G, Giannetti A, et al. One-year treatment of chronic urticaria with mizolastine: efficacy and safety. URTOL study group. J Eur Acad Dermatol Venereol. 2000 Mar;14(2):83-90.

[2]Prakash A, Lamb HM. Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria. BioDrugs. 1998 Jul;10(1):41-63.

[3]Prakash A, Lamb HM. Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria. BioDrugs. 1998 Jul;10(1):41-63

[4]Scadding GK, Tasman AJ, Murrieta-Aguttes M, Bachert C. Mizolastine is effective and well tolerated in long-term treatment of perennial allergic rhinoconjunctivitis. Riperex Study Group. J Int Med Res. 1999;27(6):273-85

[5]Taglialatela M, Pannaccione A, Castaldo P, Giorgio G, Annunziato L. Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine. Br J Pharmacol. 2000 Nov;131(6):1081-8

[6]Purohit A, Mélac M, Pauli G, Frossard N. Comparative activity of cetirizine and mizolastine on histamine-induced skin wheal and flare responses at 24 h. Br J Clin Pharmacol. 2002 Mar;53(3):250-4