181183-52-8 Usage
Description
Almotriptan is a triptan drug that belongs to the selective serotonin receptor agonists category. It is a serotonin 5HT-1B/1D-receptor agonist, specifically designed for the treatment of migraine headaches. Almotriptan has a high specificity affinity for serotonin 5-HT receptors, leading to vasoconstriction of the brain blood vessels and affecting the redistribution of blood flow. These effects stop pain signals from being sent to the brain and suppress the release of certain natural substances that cause pain, nausea, and other migraine symptoms. Marketed in 2000, it has the highest oral bioavailability among all triptans and is metabolized by both MAO-A and CYP3A4, resulting in a more favorable side effects profile compared to sumatriptan. Almotriptan is available in a 12.5 mg tablet form and is marketed under the brand name Axert (Ortho-McNeil). It is a pale yellow solid and is also known as the malate salt of almotriptan.
Uses
Used in Pharmaceutical Industry:
Almotriptan is used as an anti-migraine agent for the treatment of migraine headaches. It acts as a serotonin 5HT1B/1D-receptor agonist, leading to vasoconstriction of the brain blood vessels and affecting the redistribution of blood flow, which helps in stopping pain signals from being sent to the brain and suppressing the release of certain natural substances that cause pain, nausea, and other migraine symptoms.
Used in Migraine Treatment:
Almotriptan is used as a treatment for migraine headaches, specifically targeting the serotonin 5-HT1B and 5-HT1D receptors. It induces contractions in isolated canine saphenous veins and increases carotid vascular resistance in anesthetized cats without increasing blood pressure or heart rate. Formulations containing almotriptan have been effectively used in the treatment of migraine headaches. However,
References
https://en.wikipedia.org/wiki/Almotriptan
https://www.drugbank.ca/drugs/DB00918
Originator
Almogran ,Lundbeck
Therapeutic Function
Migraine therapy
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)
181183-52-8Relevant articles and documents
Pharmaceutical composition comprising almotriptan malate having uniform drug distribution and potency
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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
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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
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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.