ALMOTRIPTAN

ChemicalBook > CAS DataBase List > ALMOTRIPTAN

Description References

Product Name: ALMOTRIPTAN
CAS No.: 181183-52-8
Chemical Name: ALMOTRIPTAN
Synonyms: Axert;Almogran;PNU 180638;PNU-180638;Almotriptan;LAS-31416 Malate;1-[[[3-[2-(dimeth;Amotriptan malate;AlmotriptanMaleate;ALMOTRIPTAN MALATE
CBNumber: CB2417037
Molecular Formula: C21H31N3O7S
Formula Weight: 469.55
MOL File: 181183-52-8.mol

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ALMOTRIPTAN Property

Melting point:: 170-172°C
storage temp.: 2-8°C
solubility: Basic Alcohol (Very Slightly), DMSO (Slightly), Methanol (Slightly, Heated)
form: powder
color: white to beige

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Safety

HS Code: 2935904000

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H312Harmful in contact with skin

H332Harmful if inhaled

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P322Specific measures (see …on this label).

P363Wash contaminated clothing before reuse.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1210
Product name: Almotriptan malate
Purity: ≥98% (HPLC)
Packaging: 10MG
Price: $138
Updated: 2023/06/20

Sigma-Aldrich

Product number: SML1210
Product name: Almotriptan malate
Purity: ≥98% (HPLC)
Packaging: 50MG
Price: $547
Updated: 2023/06/20

Sigma-Aldrich

Product number: 1013512
Product name: Almotriptan malate
Purity: United States Pharmacopeia (USP) Reference Standard
Packaging: 200MG
Price: $400
Updated: 2022/05/15

TCI Chemical

Product number: A3111
Product name: Almotriptan Malate
Packaging: 25MG
Price: $28
Updated: 2024/03/01

TCI Chemical

Product number: A3111
Product name: Almotriptan Malate
Packaging: 100MG
Price: $74
Updated: 2024/03/01

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ALMOTRIPTAN Chemical Properties,Usage,Production

Description

Almotriptan is a kind of triptan drug which can be used for the treatment of migraine headaches. It is belong to a drug category of selective serotonin receptor agonists. It has a high and specificity affinity for serotonin 5-HT receptors, further leading to vascoconstriction of the brain blood vessel and affecting the redistribution of blood flow. These effects stop pain signals from being sent to the brain, and further suppressing the release of certain natural substances which cause pain, nausea and other migraine symptoms. However, it doesn’t prevent migraine attacks.

References

https://en.wikipedia.org/wiki/Almotriptan
https://www.drugbank.ca/drugs/DB00918

Description

Almotriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT_1B and 5-HT_1D (IC₅₀s = 12 and 13 nM, respectively, in a radioligand binding assay). It is selective for human 5-HT_1B and 5-HT_1D receptors over rat 5-HT_1A and human 5-HT_2A and 5-HT₄ receptors (IC₅₀s = 0.85, 25.1, and 140 μM, respectively). Almotriptan induces contractions in isolated canine saphenous veins (EC₅₀ = 394 nM) but not isolated rabbit renal or mesenteric arteries. It increases carotid vascular resistance in anesthetized cats (ED₁₀₀ = 11 μg/kg, i.v.) without increasing blood pressure or heart rate. Formulations containing almotriptan have been used in the treatment of migraine headaches.

Chemical Properties

Pale Yellow Solid

Originator

Almogran ,Lundbeck

Uses

Almotriptan is a serotonin 5HT-1B/1D-receptor agonist; antimigraine.

Uses

Almotriptan is a serotonin 5HT1B /1D-receptor agonist used for treatment of migraine.

Uses

anti-migraine agent

Definition

ChEBI: The malate salt of almotriptan.

Manufacturing Process

To a solution of previously dried 1-[[2-carboxy-3-(2-dimethylaminoethyl)-5- indolyl]methanesulphonyl]-pyrrolidine (1.6 g; 0.0442 moles) in anhydrous quinoline (75 ml) and under atmosphere of nitrogen, cuprous oxide (160 mg; 0.0011 moles) was added. The reaction mixture was heated to 190°C for 15 minutes, stirred to room temperature, poured into a mixture of 1 N hydrochloric acid (150 ml) and ethyl acetate (50 ml), shaken and decanted. The aqueous solution was washed several times with ethyl acetate, then solid sodium bicarbonate was added until pH = 7.8, and washed with n-hexane to eliminate the quinoline. The aqueous solution was made alkaline with solid potassium carbonate and extracted with ethyl acetate. The organic solution was dried (Na2SO4), the solvent removed under reduced pressure when a dark oil was obtained (1.3 g; yield 92%). This product was purified by column chromatography with silica gel and methylene chloride:ethanol:ammonium hydroxide (60:8:1) as eluent and a white foam (0.8 g) of 1-[[3-(2- dimethylaminoethyl)-5-indolyl]methanesulphonyl]-pyrrolidine was obtained. To a solution of the above product (0.8 g) in acetone (30 ml), a few drops of hydrogen chloride saturated dioxan solution, were added. The precipitated solid was collected by filtration, washed with acetone and dried to give 1-[(3- (2-(dimethylamino)ethyl)-5-indolyl)methanesulphonyl]-pyrrolidine hydrochloride (0.75 g). Melting point 218°-220°C.
In practice it is usually used as malate salt.

brand name

Axert (Ortho-McNeil).

Therapeutic Function

Migraine therapy

General Description

Almotriptan, marketed in 2000, has the highest oralbioavailability among all triptans. It is metabolizedby both MAO-A and CYP3A4, thus has a more favorableside effects profile when compared with sumatriptan.However, it is only available in a 12.5 mg tablet form.

Biochem/physiol Actions

Almotriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine. Almotriptan has low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors while affinity for 5-HT receptors other than 5-HT(1B/1D) is substantially lower. Affinity for 5-HT(7) and 5-HT(1A) receptors was approximately 40 and 60 times lower than that for 5-HT(1B/1D) receptors, respectively.

ALMOTRIPTAN Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from ALMOTRIPTAN manufacturers

Zibo Hangyu Biotechnology Development Co., Ltd

Product: ALMOTRIPTAN 181183-52-8
Price: US $70.00-700.00/kg
Min. Order: 10kg
Purity: 0.99
Supply Ability: 20tons
Release date: 2023-10-31

WUHAN FORTUNA CHEMICAL CO., LTD

Product: Almotriptan Malate 181183-52-8
Price: US $0.00/Kg/Bag
Min. Order: 100g
Purity: 98%min
Supply Ability: 10kg
Release date: 2021-10-20

Hebei Mingeng Biotechnology Co., Ltd

Product: Almotriptan 181183-52-8
Price: US $200.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 1000kg/Month
Release date: 2022-11-21

181183-52-8, ALMOTRIPTANRelated Search:

AlMotriptan Related CoMpound B {3-[2-(DiMethylaMino)ethyl]-5-[(pyrrolidine-1-yl)sulfonylMethyl]-1H-indol-1-yl}Methanol 1-[[[3-[2-(DiMethylaMino)ethyl]-1H-indol-5-yl]Methyl]sulfonyl]pyrrolidine Monohydrochloride Enzastaurin (LY317615) Torin 1 ABT 737 VX-661 Rapamycin Ataluren (PTC124) Enalapril maleate Empagliflozin Etretinate Epalrestat Almotriptan ALMOTRIPTAN Sumatriptan succinate Sumatriptan 3-(2-Aminoethyl)-N-methyl-1H-indole-5-methanesulfonamide

BUTANEDIOIC ACID, HYDROXY-, COMPD WITH 1-[[[3-[2-(DIMETHYLAMINO)ETHYL]-1H-INDOL-5-YL]METHYL]SULFONYL]PYRROLIDINE

ALMOTRIPTAN MALATE

AlmotriptanMaleate

1-[[[2-(Dimethyl-amino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine Malate

1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulphonyl]pyrrolidine Malate

LAS-31416 Malate

Almotriptan

1-[[[3-[2-(dimeth

2-Hydroxy-butanedioic acid, compd. with N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-indole-3-ethanamine (1:1)

hydroxy-Butanedioic acid, compd.with 1-[[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine(1:1)(9CI)

Almotriptan Malate (200 mg)

AlMotriptan Malate See: A575201

AlMotriptan Malate (Axert)

N,N-Dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]ethanamine

N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-indole-3-ethanamine,compd. with 2-hydroxy-butanedioic acid

Amotriptan malate

Almogran

Axert

AXERT; ALMOGRAN; PNU-180638;PNU 180638

PNU 180638

PNU-180638

Almotriptan Malate(PNU180638)

3-[2-(Dimethylamino)ethyl]-5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indole Malate

ALMOTRIPTAN USP/EP/BP

Almotriptan Malate (LAS 31416)

Almotriptan MaleateQ: What is Almotriptan Maleate Q: What is the CAS Number of Almotriptan Maleate Q: What is the storage condition of Almotriptan Maleate Q: What are the applications of Almotriptan Maleate

Almotriptan Malate (1013512)

Butanedioic acid, 2-hydroxy-, compd. with N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-indole-3-ethanamine (1:1)

181183-52-8

C17H25N3O2SC4H6O5

C21H31N3O7S

Inhibitors

API

Pharmaceutical material and intermeidates

Intermediates & Fine Chemicals

Neurochemicals

Pharmaceuticals