80012-43-7

80012-43-7 structure

Name: Epinastine
Chemical Name: epinastine
CAS Number: 80012-43-7
Molecular Formula: C₁₆H₁₅N₃
Molecular Weight: 249.31000
Catalog: API Antiallergic Antihistamine
Create Date: 2018-07-11 16:11:39
Modify Date: 2024-01-04 18:23:07
Epinastine(WAL801) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.Target: Histamine ReceptorEpinastine 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 [1]. 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 [2]. 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 [3]. 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 [4].

Name	epinastine
Synonyms	EPINASTINE BASE 9,13b-Dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepin-3-amine Flurinol(R) 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine Epinastine 3-Amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine MFCD00865648

Description	Epinastine(WAL801) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.Target: Histamine ReceptorEpinastine 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 [1]. 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 [2]. 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 [3]. 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 [4].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Histamine Receptor Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Inflammation/Immunology
References	[1]. Fugner, A., et al., In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung, 1988. 38(10): p. 1446-53. [2]. Roeder, T., J. Degen, and M. Gewecke, Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. Eur J Pharmacol, 1998. 349(2-3): p. 171-7. [3]. Kamei, C., et al., Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol, 1992. 14(1-2): p. 191-205. [4]. Kohyama, T., et al., A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun, 1997. 230(1): p. 125-8.

Density	1.32 g/cm3
Boiling Point	428ºC at 760 mmHg
Melting Point	270ºC
Molecular Formula	C₁₆H₁₅N₃
Molecular Weight	249.31000
Flash Point	212.7ºC
Exact Mass	249.12700
PSA	41.62000
LogP	2.66770
Index of Refraction	1.727
Storage condition	2-8℃

Material Safety Data Sheet

Section1. Identiﬁcation of the substance
Product Name: Epinastine
Synonyms:

Section2. Hazards identiﬁcation
Harmful by inhalation, in contact with skin, and if swallowed.

Section3. Composition/information on ingredients.
Ingredient name:Epinastine
CAS number:80012-43-7

Section4. First aid measures
Skin contact:Immediately wash skin with copious amounts of water for at least 15 minutes while removing
contaminated clothing and shoes. If irritation persists, seek medical attention.
Eye contact:Immediately wash skin with copious amounts of water for at least 15 minutes. Assure adequate
ﬂushing of the eyes by separating the eyelids with ﬁngers. If irritation persists, seek medical
attention.
Inhalation:Remove to fresh air. In severe cases or if symptoms persist, seek medical attention.
Ingestion:Wash out mouth with copious amounts of water for at least 15 minutes. Seek medical attention.

Section5. Fire ﬁghting measures
In the event of a ﬁre involving this material, alone or in combination with other materials, use dry
powder or carbon dioxide extinguishers. Protective clothing and self-contained breathing apparatus
should be worn.

Section6. Accidental release measures
Personal precautions: Wear suitable personal protective equipment which performs satisfactorily and meets local/state/national
standards.
Respiratory precaution:Wear approved mask/respirator
Hand precaution:Wear suitable gloves/gauntlets
Skin protection:Wear suitable protective clothing
Eye protection:Wear suitable eye protection
Methods for cleaning up: Mix with sand or similar inert absorbent material, sweep up and keep in a tightly closed container
for disposal. See section 12.
Environmental precautions: Do not allow material to enter drains or water courses.

Section7. Handling and storage
Handling:This product should be handled only by, or under the close supervision of, those properly qualiﬁed
in the handling and use of potentially hazardous chemicals, who should take into account the ﬁre,
health and chemical hazard data given on this sheet.
Store in closed vessels.
Storage:

Section8. Exposure Controls / Personal protection
Engineering Controls: Use only in a chemical fume hood.
Personal protective equipment: Wear laboratory clothing, chemical-resistant gloves and safety goggles.
General hydiene measures: Wash thoroughly after handling. Wash contaminated clothing before reuse.

Section9. Physical and chemical properties
Appearance:Not speciﬁed
Boiling point:No data
No data
Melting point:
Flash point:No data
Density:No data
Molecular formula:C16H15N3
Molecular weight:249.3

Section10. Stability and reactivity
Conditions to avoid: Heat, ﬂames and sparks.
Materials to avoid: Oxidizing agents.
Possible hazardous combustion products: Carbon monoxide, nitrogen oxides.

Section11. Toxicological information
No data.

Section12. Ecological information
No data.

Section13. Disposal consideration
Arrange disposal as special waste, by licensed disposal company, in consultation with local waste
disposal authority, in accordance with national and regional regulations.

Section14. Transportation information
Non-harzardous for air and ground transportation.

Section15. Regulatory information
No chemicals in this material are subject to the reporting requirements of SARA Title III, Section
302, or have known CAS numbers that exceed the threshold reporting levels established by SARA
Title III, Section 313.

SECTION 16 - ADDITIONAL INFORMATION
N/A

127786-29-2

~93%

80012-43-7

Literature: USV LIMITED Patent: WO2009/63504 A2, 2009 ; Location in patent: Page/Page column 25 ;

127785-96-0

80012-43-7

Literature: WO2009/63504 A2, ; Page/Page column 24 ;

Precursor 2
127786-29-2 127785-96-0
DownStream 1
108929-04-0

80012-43-7	108929-04-0
80012-44-8	1217052-16-8
127786-29-2	141342-71-4
80012-42-6	141342-69-0
141342-70-3	80012-45-9
1158522-08-7	1384954-59-9
940364-43-2	134104-43-1
131615-57-1	6906-52-1
930439-75-1	1018584-77-4
2137101-11-0	1375289-11-4