ELESTAT
Epinastine
CAS: 80012-43-7
Molecular Formula: C16H15N3
ELESTAT - Names and Identifiers
| Name | Epinastine |
| Synonyms | WAL801 CS-1366 ELESTAT Epinastine EPINASTINE Apinastine Base EPINASTINE BASE Epinastine base 3-amino-9,13b-dihydro-1h-dibenz[c,f]imidazo[1,5-a]azepine 9,13b-Dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepin-3- amine 9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine 3-Amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine |
| CAS | 80012-43-7 |
| EINECS | 616-785-3 |
| InChI | InChI=1/C16H15N3/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) |
ELESTAT - Physico-chemical Properties
| Molecular Formula | C16H15N3 |
| Molar Mass | 249.31 |
| Density | 1.32±0.1 g/cm3(Predicted) |
| Melting Point | 205-208° |
| Boling Point | 428.0±55.0 °C(Predicted) |
| Flash Point | 212.7°C |
| Vapor Presure | 1.56E-07mmHg at 25°C |
| pKa | 11.2(at 25℃) |
| Storage Condition | Keep in dark place,Inert atmosphere,Room temperature |
| Refractive Index | 1.727 |
| In vitro study | Epinastine is able to displace specific [ 3 H]NC-5Z binding at low concentrations in the locust nervous tissue. Epinastine binds to the honey bees neuronal octopamine receptor with K i 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 Ca 2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca 2+ 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 vivo study | Epinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs. |
ELESTAT - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 4.011 ml | 20.055 ml | 40.111 ml |
| 5 mM | 0.802 ml | 4.011 ml | 8.022 ml |
| 10 mM | 0.401 ml | 2.006 ml | 4.011 ml |
| 5 mM | 0.08 ml | 0.401 ml | 0.802 ml |
Last Update：2024-01-02 23:10:35
ELESTAT - Reference Information
| biological activity | Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective, orally active histamine H1 receptor antagonist. Epinastine also inhibits the release by IL-8 and has an anti-allergic effect. |
| in vitro study | Epinastine is able to place specific [3 H]NC-5Z binding at low concentrations in the locust nervous tissue. Epinastine binds to the honey bees neuronal octopamine receptor with K I 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 Ca 2 uptake into lung mast cells in actively sensitized guinea pigs but also Ca 2 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 vivo studies | Epinastine shows a high affinity to H1-receptors in receptor binding studies in the quinea pig ileum. Epinastine inhibitors-induced reactions in the skin or the lung of rats, dogs and guinea pigs. |
Last Update：2024-04-09 21:01:54
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