Description References
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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
Water Solubility 
H2O: 10mg/mL, clear
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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
$146
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1210
Product name
Almotriptan malate
Purity
≥98% (HPLC)
Packaging
50MG
Price
$577
Updated
2025/07/31
Sigma-Aldrich
Product number
1013512
Product name
Almotriptan malate
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
200MG
Price
$376
Updated
2025/07/31
TCI Chemical
Product number
A3111
Product name
Almotriptan Malate
Packaging
25MG
Price
$28
Updated
2025/07/31
TCI Chemical
Product number
A3111
Product name
Almotriptan Malate
Packaging
100MG
Price
$74
Updated
2025/07/31
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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-HT1B and 5-HT1D (IC50s = 12 and 13 nM, respectively, in a radioligand binding assay). It is selective for human 5-HT1B and 5-HT1D receptors over rat 5-HT1A and human 5-HT2A 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.

References

[1] Patent: WO2010/113183, 2010, A2. Location in patent: Page/Page column 26
[2] Patent: WO2008/151584, 2008, A1. Location in patent: Page/Page column 4; 11-12
[3] Patent: EP2774605, 2014, A1. Location in patent: Paragraph 0107
[4] Patent: WO2009/16414, 2009, A1. Location in patent: Page/Page column 13-15; 19-20
[5] Patent: US2007/112055, 2007, A1. Location in patent: Page/Page column 7

ALMOTRIPTAN Preparation Products And Raw materials

Raw materials

Preparation Products

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ALMOTRIPTAN Suppliers

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View Lastest Price from ALMOTRIPTAN manufacturers

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
Moxin Chemicals
Product
Almotriptan Malate 181183-52-8
Price
US $0.00-0.00/mg
Min. Order
10mg
Purity
95
Supply Ability
1000000
Release date
2025-02-14
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

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)
  • 1-[[[3-[2- (Dimethylamino) ethyl] - 1H- indol-5-yl] sulfonyl] pyrrolidine. Malate
  • Almotriptan Malate, 10 mM in DMSO
  • 181183-52-8
  • C17H25N3O2SC4H6O5
  • C21H31N3O7S
  • Inhibitors
  • API
  • Pharmaceutical material and intermeidates
  • Intermediates & Fine Chemicals
  • Neurochemicals
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