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Epinastine HCl(WAL801)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Epinastine HCl(WAL801)图片
CAS NO:108929-04-0
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)285.77
FormulaC16H15N3.HCl
CAS No.108929-04-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 57 mg/mL (199.5 mM)
Water: N/A
Ethanol: 57 mg/mL (199.5 mM)
Solubility (In vivo)

Chemical Name: 3-Amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine Hydrochloride

InChi Key: VKXSGUIOOQPGAF-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H15N3.ClH/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16;/h1-8,15H,9-10H2,(H2,17,18);1H

SMILES Code: C1C2C3=CC=CC=C3CC4=CC=CC=C4N2C(=N1)N.Cl

SynonymsWAL-801CL HCl; WAL801CL HCl; Alesion; Elestat; Epinastine HCl; Epinastin HCl; WAL 801CL HCl; WAL-801-CL HCl; Epinastine Hydrochloride;
实验参考方法
In Vitro

In vitro activity: Epinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. Epinastine is able to displace specific [3H]NC-5Z binding at low concentrations in the locust nervous tissue. Epinastine binds to the honey bees neuronal octopamine receptor with Ki of 1.1 nM. Epinastine antagonises octopamine-induced cAMP formation in the insect brain. Epinastine causes an inhibition of histamine release from rat peritoneal mast cells induced by both antigen-antibody reaction and compound 48/80. Epinastine is similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. Epinastine is effective in inhibiting not only Ca2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca2+ release from the intracellular Ca store of rat peritoneal mast cells exposed to both compound 48/80 and substance P. Epinastine shows a dose- and time-dependent suppressive effect on IL-8, one of the chemokines for eosinophils, released from eosinophils isolated from atopic diseases.

In VivoEpinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs.
Animal model
Formulation & Dosage
References

J Pharmacol Exp Ther. 1997 Apr;281(1):233-44; Drugs. 1996;52 Suppl 1:15-9; Drugs. 1996;52 Suppl 1:8-14.