Emedastine
Emedastine Basic information
- Product Name:
- Emedastine
- Synonyms:
-
- EMEDASTINE
- 1-(2-Ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)benzimidazole
- 1-(2-Ethoxyethyl)-2-(4-methylhexahydro-1H-1,4-diazepine-1-yl)-1H-benzimidazole
- 1-(2-Ethoxyethyl)-2-[(hexahydro-4-methyl-1H-1,4-diazepin)-1-yl]-1H-benzimidazole
- 1-(2-ethoxyethyl)-2-(4-Methyl-1,4-diazepan-1-yl)-1H-1,3-benzodiazole
- 1-(2-Ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzimidazole
- 1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzo[d]imidazole
- Emedastine impurity F
- CAS:
- 87233-61-2
- MF:
- C17H26N4O
- MW:
- 302.41
- EINECS:
- 200-258-5
- Product Categories:
-
- impurity
- DCP
- GYL
- Mol File:
- 87233-61-2.mol
Emedastine Chemical Properties
- Boiling point:
- 446.6±55.0 °C(Predicted)
- Density
- 1.15±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: 125 mg/mL (413.35 mM); Ethanol: 100 mg/mL (330.68 mM)
- pka
- 8.86±0.10(Predicted)
- form
- Viscous Liquid
- color
- Yellow to brown
- CAS DataBase Reference
- 87233-61-2(CAS DataBase Reference)
Emedastine Usage And Synthesis
Uses
Antihistaminic, H1-receptor; asthma prophylactic; anti-allergic.
Definition
ChEBI: 1-Methyl-1,4-diazepane in which the hydrogen attached to the nitrogen at position 4 is substituted by a 1-(2-ethoxyethyl)-1H-benzimidazol-2-yl group. A relatively selective histamine H1 antagonist, it is used as the ifumatate salt for allergic rhinitis, urticaria, and pruritic skin disorders, and in eyedrops for the symptomatic relief of allergic conjuntivitis.
brand name
Emadine (Alcon).
Clinical Use
Emedastine also is a newer antihistamine used topically in the eye for conjunctivitis. It has very high H1 receptor selectivity characteristics, and it is structurally related to the benzimidazoles, such as astemizole. Inhibition of mast cell release of inflammatory mediators has been noted.
in vivo
Emedastine (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg[3].
Pretreatment with Emedastine (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B[3].
Emedastine (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs[2].
Emedastine inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM)[2].
| Animal Model: | Male ICR mice 5-6 weeks of age[3] |
| Dosage: | 0.03, 0.1, 0.3 mg/kg |
| Administration: | Orally; 30 min before pruritogen injection |
| Result: | Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3 mg/kg. |
IC 50
H1 Receptor: 1.3 nM (Ki); H2 Receptor: 49067 nM (Ki); H3 Receptor: 12430 nM (Ki)
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