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CAS NO.90729-43-4
| Ebastine Basic information |
| Product Name: | Ebastine |
| Synonyms: | 4-(4-benzhydryloxy-1-piperidyl)-1-(4-tert-butylphenyl)butan-1-one;EBASTEL;EBASTIN;EBASTINE;EVASTEL;KESTINE;1-(4-(1,1-dimethylethyl)phenyl)-4-(4-(diphenylmethoxy)-1-piperidinyl)-1-buta;1-butanone,1-(4-(1,1-dimethylethyl)phenyl)-4-(4-(diphenylmethoxy)-1-piperidiny |
| CAS: | 90729-43-4 |
| MF: | C32H39NO2 |
| MW: | 469.66 |
| EINECS: | |
| Product Categories: | Active Pharmaceutical Ingredients;Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitors |
| Mol File: | 90729-43-4.mol |
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|
|
| Ebastine Chemical Properties |
| mp | 80-82°C |
| storage temp. | Room temp |
| CAS DataBase Reference | 90729-43-4(CAS DataBase Reference) |
| Safety Information |
| RTECS | EL8140000 |
| Ebastine Usage And Synthesis |
| Antihistamines |
Antihistamines are class of drugs which are able to compete histamine receptors on cells with histamine , which makes histamine can not be combined with histamine receptors, resulting in an anti-histamine effect , according to the different types of histamine receptors, antihistamines can be divided into H1 receptor blockers and H2 receptor blockers, H1 receptor antagonists are antihistamines that are generally referred to in the past, which can antagonize the relaxation of vascular and smooth muscle contraction action of histamine and help to alleviate or eliminate allergy symptoms caused by endogenous release of histamine.It is mainly used for prevention and treatment of skin and mucous allergic diseases, motion sickness and vomiting. Ebastine and cetirizine, loratadine, cetirizine L, mizolastine are several currently used anti-H1 receptor antihistamines which are non-sedating ,they are anti-allergic drugs, which is characterized by the central nervous non-sedating or little sedating ,their anti-histamine effect is stronger, which can significantly inhibit flush and wind group caused by the histamine , it does not affect the mast cells to release histamine. This product starts effect 1 to 4 hours after oral administration , time to peak plasma concentration is 3 to 6 hours, it can go through the blood-brain barrier, it is converted to an active form carebastine in vivo. Healthy adult volunteers after once po ebastine, Tmax is about 3 ~ 6 h, 3 ~ 5 times / d administration can make plasma concentrations reach steady state. After single serving 10 mg, Cmax is approximately 0.1mg / L. Administration with food may increase its bioavailability. PPB is about 98%. Vd is about 90 ~ 140 L. Terminal T1 / 2 is 13 ~ 16h, it is mainly excreted in the urine. The main clinical uses are for the treatment of various allergic diseases such as chronic idiopathic urticaria, seasonal, perennial allergic rhinitis, skin pruritus. Adult treatment of chronic urticaria, or allergic rhinitis, po, 10 mg, qd; the amount of children is 5 mg, qd. Large doses of ebastine 20 mg, qd are only for more severe allergic diseases in adults, and Administration in the morning will achieve better results. The most common adverse events are somnolence, headache, dry mouth, most patients have mild to moderate reactions,which does not affect the uses. Other rare adverse reactions are fatigue, nausea, vomiting, loss of appetite, hyperactivity, diarrhea, constipation and upset. Up to 1 year or more use of drugs observation, the most common adverse reactions are headache and gastrointestinal disorders. The above information is edited by the chemicalbook of Tian Ye. |
| Chemical Properties | Ebastine Fumarate: Crystallize from ethanol, mp 197-198 ℃. Acute toxicity LD50 rodent (mg / kg): 500 intraperitoneal injection;> 4,000 oral. |
| Application | Its antihistamine activity is competitive at low concentrations,while it is non-competitive at high concentrations. It is used for allergic diseases, including children allergic rhinitis , adults year-round rhinitis, seasonal rhinitis, hay fever and chronic urticaria. |
| Chemical Properties | White to Off-White Powder |
| Usage | A nonsedating type histamine H1-receptor antagonist. Antihistaminic |
| Ebastine Preparation Products And Raw materials |
| Raw materials | 4-Hydroxypiperidine -->Bromodiphenylmethane |
| Ebastine Basic information |
| Product Name: | Ebastine |
| Synonyms: | 4-(4-benzhydryloxy-1-piperidyl)-1-(4-tert-butylphenyl)butan-1-one;EBASTEL;EBASTIN;EBASTINE;EVASTEL;KESTINE;1-(4-(1,1-dimethylethyl)phenyl)-4-(4-(diphenylmethoxy)-1-piperidinyl)-1-buta;1-butanone,1-(4-(1,1-dimethylethyl)phenyl)-4-(4-(diphenylmethoxy)-1-piperidiny |
| CAS: | 90729-43-4 |
| MF: | C32H39NO2 |
| MW: | 469.66 |
| EINECS: | |
| Product Categories: | Active Pharmaceutical Ingredients;Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitors |
| Mol File: | 90729-43-4.mol |
|
|
|
| Ebastine Chemical Properties |
| mp | 80-82°C |
| storage temp. | Room temp |
| CAS DataBase Reference | 90729-43-4(CAS DataBase Reference) |
| Safety Information |
| RTECS | EL8140000 |
| Ebastine Usage And Synthesis |
| Antihistamines |
Antihistamines are class of drugs which are able to compete histamine receptors on cells with histamine , which makes histamine can not be combined with histamine receptors, resulting in an anti-histamine effect , according to the different types of histamine receptors, antihistamines can be divided into H1 receptor blockers and H2 receptor blockers, H1 receptor antagonists are antihistamines that are generally referred to in the past, which can antagonize the relaxation of vascular and smooth muscle contraction action of histamine and help to alleviate or eliminate allergy symptoms caused by endogenous release of histamine.It is mainly used for prevention and treatment of skin and mucous allergic diseases, motion sickness and vomiting. Ebastine and cetirizine, loratadine, cetirizine L, mizolastine are several currently used anti-H1 receptor antihistamines which are non-sedating ,they are anti-allergic drugs, which is characterized by the central nervous non-sedating or little sedating ,their anti-histamine effect is stronger, which can significantly inhibit flush and wind group caused by the histamine , it does not affect the mast cells to release histamine. This product starts effect 1 to 4 hours after oral administration , time to peak plasma concentration is 3 to 6 hours, it can go through the blood-brain barrier, it is converted to an active form carebastine in vivo. Healthy adult volunteers after once po ebastine, Tmax is about 3 ~ 6 h, 3 ~ 5 times / d administration can make plasma concentrations reach steady state. After single serving 10 mg, Cmax is approximately 0.1mg / L. Administration with food may increase its bioavailability. PPB is about 98%. Vd is about 90 ~ 140 L. Terminal T1 / 2 is 13 ~ 16h, it is mainly excreted in the urine. The main clinical uses are for the treatment of various allergic diseases such as chronic idiopathic urticaria, seasonal, perennial allergic rhinitis, skin pruritus. Adult treatment of chronic urticaria, or allergic rhinitis, po, 10 mg, qd; the amount of children is 5 mg, qd. Large doses of ebastine 20 mg, qd are only for more severe allergic diseases in adults, and Administration in the morning will achieve better results. The most common adverse events are somnolence, headache, dry mouth, most patients have mild to moderate reactions,which does not affect the uses. Other rare adverse reactions are fatigue, nausea, vomiting, loss of appetite, hyperactivity, diarrhea, constipation and upset. Up to 1 year or more use of drugs observation, the most common adverse reactions are headache and gastrointestinal disorders. The above information is edited by the chemicalbook of Tian Ye. |
| Chemical Properties | Ebastine Fumarate: Crystallize from ethanol, mp 197-198 ℃. Acute toxicity LD50 rodent (mg / kg): 500 intraperitoneal injection;> 4,000 oral. |
| Application | Its antihistamine activity is competitive at low concentrations,while it is non-competitive at high concentrations. It is used for allergic diseases, including children allergic rhinitis , adults year-round rhinitis, seasonal rhinitis, hay fever and chronic urticaria. |
| Chemical Properties | White to Off-White Powder |
| Usage | A nonsedating type histamine H1-receptor antagonist. Antihistaminic |
| Ebastine Preparation Products And Raw materials |
| Raw materials | 4-Hydroxypiperidine -->Bromodiphenylmethane |