product name Epinastine HCl
Description: Epinastine HCl (also known as WAL-801CL HCl) is an antihistamine without sedative activity and a mast cell stabilizer that is used in eye drops for the treatment of allergic conjunctivitis. Epinastine hydrochloride blocks the histamine H1 receptor and inhibits the release of histamine from mast cells. This prevents the typical allergic symptoms that are caused by histamine activity on capillaries, skin, mucous membranes.
References: Arzneimittelforschung. 1988 Oct;38(10):1446-53; Eur J Pharmacol. 1998 May 22;349(2-3):171-7.
285.77
Formula
C16H15N3.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:
Ethanol: 57 mg/mL (199.5 mM)
Solubility (In vivo)
Synonyms
WAL-801CL HCl
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19426
| 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Epinastine 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. |
