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181183-52-8

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181183-52-8 Usage

Description

Different sources of media describe the Description of 181183-52-8 differently. You can refer to the following data:
1. 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.
2. 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.

References

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

Chemical Properties

Pale Yellow Solid

Originator

Almogran ,Lundbeck

Uses

Different sources of media describe the Uses of 181183-52-8 differently. You can refer to the following data:
1. Almotriptan is a serotonin 5HT-1B/1D-receptor agonist; antimigraine.
2. Almotriptan is a serotonin 5HT1B /1D-receptor agonist used for treatment of migraine.
3. anti-migraine agent

Definition

ChEBI: The malate salt of almotriptan.

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.

Check Digit Verification of cas no

The CAS Registry Mumber 181183-52-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,8,1,1,8 and 3 respectively; the second part has 2 digits, 5 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 181183-52:
(8*1)+(7*8)+(6*1)+(5*1)+(4*8)+(3*3)+(2*5)+(1*2)=128
128 % 10 = 8
So 181183-52-8 is a valid CAS Registry Number.
InChI:InChI=1/C17H25N3O2S.C4H6O5/c1-19(2)10-7-15-12-18-17-6-5-14(11-16(15)17)13-23(21,22)20-8-3-4-9-20;5-2(4(8)9)1-3(6)7/h5-6,11-12,18H,3-4,7-10,13H2,1-2H3;2,5H,1H2,(H,6,7)(H,8,9)

181183-52-8 Well-known Company Product Price

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  • (Code)Product description
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  • USP

  • (1013512)  Almotriptan malate  United States Pharmacopeia (USP) Reference Standard

  • 181183-52-8

  • 1013512-200MG

  • 4,647.24CNY

  • Detail
  • Sigma

  • (SML1210)  Almotriptan malate  ≥98% (HPLC)

  • 181183-52-8

  • SML1210-10MG

  • 1,232.01CNY

  • Detail
  • Sigma

  • (SML1210)  Almotriptan malate  ≥98% (HPLC)

  • 181183-52-8

  • SML1210-50MG

  • 4,966.65CNY

  • Detail

181183-52-8SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 14, 2017

Revision Date: Aug 14, 2017

1.Identification

1.1 GHS Product identifier

Product name almotriptan malate

1.2 Other means of identification

Product number -
Other names N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]ethanamine,2-hydroxybutanedioic acid

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:181183-52-8 SDS

181183-52-8Synthetic route

malic acid
617-48-1

malic acid

almotriptan
154323-57-6

almotriptan

almotriptan malate
181183-52-8

almotriptan malate

Conditions
ConditionsYield
In methanol for 1h; Product distribution / selectivity; Reflux;99.51%
In methanol at 40℃;93%
In methanol at 20 - 40℃; for 2h; Large scale;93%
almotriptan 2-hydroxy benzoate
922735-96-4

almotriptan 2-hydroxy benzoate

malic acid
617-48-1

malic acid

almotriptan malate
181183-52-8

almotriptan malate

Conditions
ConditionsYield
Stage #1: almotriptan 2-hydroxy benzoate With ammonia In methanol; water; ethyl acetate for 1h;
Stage #2: malic acid In methanol at 25℃; for 4.5h; Product distribution / selectivity; Heating / reflux;
Stage #1: almotriptan 2-hydroxy benzoate With ammonia In water; ethyl acetate at 25 - 30℃; for 1h;
Stage #2: malic acid In methanol at 25 - 30℃; for 4.5h; Product distribution / selectivity; Heating / reflux;
N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonyl-methyl)-1H-indol-3-yl]-ethanaminium semioxalate
922735-94-2

N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonyl-methyl)-1H-indol-3-yl]-ethanaminium semioxalate

malic acid
617-48-1

malic acid

almotriptan malate
181183-52-8

almotriptan malate

Conditions
ConditionsYield
Stage #1: N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonyl-methyl)-1H-indol-3-yl]-ethanaminium semioxalate With ammonia In water; ethyl acetate for 1h;
Stage #2: malic acid In methanol at 20℃; for 4.5h; Product distribution / selectivity; Heating / reflux;
Stage #1: N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonyl-methyl)-1H-indol-3-yl]-ethanaminium semioxalate With ammonia In water; ethyl acetate for 1h;
Stage #2: malic acid In methanol at 25 - 35℃; for 4.5h; Product distribution / selectivity; Heating / reflux;

181183-52-8Downstream Products

181183-52-8Relevant articles and documents

Pharmaceutical composition comprising almotriptan malate having uniform drug distribution and potency

-

Paragraph 0107, (2014/09/29)

The present invention relates to tablets comprising almotriptan malate and mannitol, wherein the mannitol is in crystalline form and the bulk density of the mannitol is below 0.75 g/ml. The present invention also relates to a specific crystalline form of

NOVEL PROCESS

-

Page/Page column 13-15; 19-20, (2009/03/07)

The present invention relates to a novel process for the preparation of almotriptan and pharmaceutically acceptable salts thereof, which affords product conveniently and efficiently with commercially acceptable yields and purity. The present invention also relates to a novel synthetic intermediate used in the process.

METHOD FOR THE PREPARATION OF HIGH PURITY ALMOTRIPTAN

-

Page/Page column 4; 11-12, (2009/01/24)

A method for the preparation and purification of the substance of formula (I), i.e. 3-[2- (dimethylamino)ethyl]-5-(1-pyrrolidinylsulfonylmethyl)-1H-indole, which comprises (a) conversion of 4-(1-pyrrolidinylsulfonylmethyl)phenylhydrazine of formula (III) by reaction with an organic or inorganic acid to a salt that is insoluble or poorly soluble in water, which is converted to 3-(2-aminoethyl)-5-(1-pyrrolidinylsulfonylmethyl)indole of formula (VII), which is further converted without isolation to a solution of the almotriptan base, which provides a crystalline salt of almotriptan with an organic or inorganic acid; (b) conversion of the salt of almotriptan to the almotriptan base, which separates from the solution in the crystalline form; (c) purification of the almotriptan base by crystallization from an organic solvent.

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