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Azelastine

Azelastine ??? ???
?? ??:
58581-89-8
???:
Azelastine
???(??):
-4-yl)-;AZELASTINE;SPBio_000657;KBio3_002992;CAS 790307-93-0;Azelastine base;Spectrum3_001984;Spectrum2_000649;Azeptin:Rhino1ast;Azelastine USP/EP/BP
CBNumber:
CB6256007
???:
C22H24ClN3O
??? ??:
381.9
MOL ??:
58581-89-8.mol

Azelastine ??

???
111 - 115°C
?? ?
533.9±60.0 °C(Predicted)
??
1.1505 (rough estimate)
???
1.5790 (estimate)
?? ??
2-8°C
???
?????(?? ???), DMSO(?? ???, ??), ???(?? ???)
?? ?? (pKa)
pKa 9.82(H2O t=25 I=0.025) (Uncertain)
??? ??
??
??? ??
??? ??
??
???? ?????
BCS Class
1
???
Stable under recommended storage conditions., Stable Under Recommended Storage C
InChI
InChI=1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3
InChIKey
MBUVEWMHONZEQD-UHFFFAOYSA-N
SMILES
C1(=O)C2=C(C=CC=C2)C(CC2=CC=C(Cl)C=C2)=NN1C1CCCN(C)CC1
CAS ??????
58581-89-8(CAS DataBase Reference)
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
?? ?? ??? 58581-89-8(Hazardous Substances Data)
?? LD50 orl-rat: 310 mg/kg ARZNAD 31,1184,81
????(GHS): Exclamation Mark (GHS07)
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H302 ??? ??? ?? ?? ?? - ?? ?? 4 ?? P264, P270, P301+P312, P330, P501
H312 ??? ???? ??? ?? ?? ?? - ?? ?? 4 ?? P280,P302+P352, P312, P322, P363,P501
H315 ??? ??? ??? ????? ?? ????? ?? 2 ?? P264, P280, P302+P352, P321,P332+P313, P362
H332 ???? ??? ?? ?? ?? ?? ?? 4 ?? P261, P271, P304+P340, P312
H335 ?? ???? ??? ? ?? ?? ???? ?? - 1? ??;???? ?? ?? 3 ??
??????:
P261 ??·?·??·???·??·...·????? ??? ????.
P264 ?? ??? ?? ??? ????.
P264 ?? ??? ?? ??? ????.
P270 ? ??? ??? ??? ???, ???? ???? ???.
P271 ?? ?? ??? ? ?? ???? ?????.
P280 ????/???/???/?????? ?????.
P301+P312 ??? ???? ??? ????(??)? ??? ????.
P302+P352 ??? ??? ??? ?? ????.
P304+P340 ???? ??? ??? ?? ??? ??? ???? ?? ??? ??? ????.
P312 ???? ??? ????(??)? ??? ????.
P321 (…) ??? ???.
P322 ?? ??(??? … ??)
P330 ?? ?????.
P332+P313 ?? ??? ??? ???? ??· ??? ????.
P362 ??? ??? ?? ?? ?? ?????
P363 ?? ??? ??? ??? ?????.
P501 ...? ??? / ??? ?? ???.

Azelastine C??? ??, ??, ??

??

anesthetic, anticonvulsant

??

ChEBI: A phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position.

Clinical Use

Azelastine, although not a close structural analogue to the benzimidazoles, has some structural similarities to them. It is used as a nasal spray for allergic rhinitis and as eye drops for allergic conjunctivitis.Like olopatadine, azelastine also stabilizes mast cells, preventing degranulation and subsequent release of histamine, leukotrienes, and PGD2. It is available in Europe for systemic use in the treatment of asthma and seasonal allergies. Besides antihistaminic effects, it also may block release of histamine and other inflammatory mediators from mast cells. When administered orally, the N-dealkylated metabolite appears to contribute significantly to its pharmacological effects.

Safety Profile

Poison by ingestion,subcutaneous, intravenous, and intraperitoneal routes.Experimental reproductive effects. When heated todecomposition it emits toxic fumes of NOx and Cl- .

Azelastine ?? ?? ? ???

???

?? ??


Azelastine ?? ??

???( 172)?? ??
??? ?? ??? ?? ?? ? ??
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Azelastine ?? ??:

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