3978-86-7 Usage
Description
Azatadine Maleate (200 MG) is a potent, long-acting antihistaminic with antiserotonin activity, used primarily for the treatment of allergic symptoms. It is a white solid and is known by the brand names Optimine (Schering) and Verban. In early testing, it has shown more than three times the potency of chlorpheniramine in the isolated guinea pig ileum screen and more than seven times the oral potency of chlorpheniramine in protecting guinea pigs against a double lethal dose of intravenously administered histamine.
Uses
Used in Pharmaceutical Industry:
Azatadine Maleate (200 MG) is used as an antihistaminic for the treatment of allergic symptoms such as rhinitis, urticaria, and pruritus. It works by blocking the action of histamine, a substance in the body that causes allergic symptoms.
Used in Allergy Treatment:
Azatadine Maleate (200 MG) is used as a medication for the relief of symptoms associated with allergic reactions, such as sneezing, itching, and runny nose. Its long-acting properties make it an effective choice for managing these symptoms over an extended period.
Used in Serotonin Antagonism:
Azatadine Maleate (200 MG) is used as a serotonin antagonist, which helps in reducing the effects of serotonin, a neurotransmitter that can cause allergic reactions and other symptoms. This dual action of antihistamine and antiserotonin makes it a versatile drug in the treatment of various allergic conditions.
Originator
Idulian,Unilabo,France,1968
Manufacturing Process
Preparation of 4-aza-5-(N-methyl-4-piperidyl)-10,11-dihydro-5Hdibenzo[
a,d]cycloheptene-5-ol: Add 17.4 g of N-methyl-4-chloropiperidine to a
stirred mixture containing 3.2 g of magnesium, 20 ml of anhydrous
tetrahydrofuran, 1 ml of ethyl bromide and a crystal of iodine. Reflux for two
hours, cool to 30-35°C and add a solution of 13 g of 4-aza-10,11-dihydro-5Hdibenzo[
a,d]cycloheptene-5-one in 25 ml of tetrahydrofuran. Stir for five
hours, remove the solvent by distillation in vacuum and add 250 ml of ether.
Add 100 ml of 10% ammonium chloride solution and extract the mixture with
chloroform. Concentrate the chloroform solution to a residue and recrystallize
from isopropyl ether obtaining 20 g of the carbinol, MP 173-174°C.
Preparation of 4-aza-5-(N-methyl-4-piperidylidene)-10,11-dihydro-5Hdibenzo[
a,d]cycloheptene: Heat 5.4 g of the carbinol and 270 g of
polyphosphoric acid for 12 hours at 140-170°C. Pour into ice water and make
alkaline with sodium hydroxide. Extract with ether. Dry ether solution and
concentrate to a residue. Crystallize from isopropyl ether, MP 124-126°C.
Preparation of 4-aza-5-(N-methyl-4-piperidylidene)-10,11-dihydro-5Hdibenzo[
a,d]cycloheptene dimaleate: To a solution containing 4.3 g of 4-aza-
(N-methyl-4-piperidylidene)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene in 55
ml of ethyl acetate, add a solution of 3.45 g of maleic acid dissolved in ethyl
acetate. Filter the resulting precipitate and recrystallize the desired product
from an ethyl acetate-methanol mixture to yield 4-aza-5-(N-methyl-4-
piperidylidene)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene dimaleate, MP
152-154°C.
Therapeutic Function
Antihistaminic
Check Digit Verification of cas no
The CAS Registry Mumber 3978-86-7 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 3,9,7 and 8 respectively; the second part has 2 digits, 8 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 3978-86:
(6*3)+(5*9)+(4*7)+(3*8)+(2*8)+(1*6)=137
137 % 10 = 7
So 3978-86-7 is a valid CAS Registry Number.
InChI:InChI=1/C20H22N2.2C4H4O4/c1-22-13-10-16(11-14-22)19-18-7-3-2-5-15(18)8-9-17-6-4-12-21-20(17)19;2*5-3(6)1-2-4(7)8/h2-7,12H,8-11,13-14H2,1H3;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1-
