Almotriptan Malate | CAS#181183-52-8 | 154323-57-6 | Serotonin Receptor Agonist

Almotriptan Malate
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 317170

CAS#: 181183-52-8(Almotriptan Malate)

Description: Almotriptan Malate is a triptan drug discovered and developed by Almirall for the treatment of heavy migraine headache. Almotriptan is a Serotonin-1b and Serotonin-1d Receptor Agonist. Binding of the drug to the receptor leads to vasoconstriction of the cranial blood vessels and thus affects the redistribution of cranial blood flow. Almotriptan significantly increases cerebral blood flow and reduces blood flow through extracerebral cranial vessels. Even though it affects cranial blood vessels a single dose of almotriptan (12.5 mg) has no clinically significant effect on blood pressure or heart rate in both young and elderly healthy volunteers.

Chemical Structure

Almotriptan Malate

CAS# 181183-52-8(Almotriptan Malate)

Instruction

Theoretical Analysis

MedKoo Cat#: 317170
Name: Almotriptan Malate
CAS#: 181183-52-8(Almotriptan Malate)
Chemical Formula: C17H25N3O2S
Exact Mass: 335.17
Molecular Weight: 335.460
Elemental Analysis: C, 60.87; H, 7.51; N, 12.53; O, 9.54; S, 9.56

Price and Availability

Size	Price	Availability
10mg	USD 250	2 Weeks
25mg	USD 450	2 Weeks
50mg	USD 750	2 Weeks
100mg	USD 1250	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 181183-52-8(Almotriptan Malate) 154323-57-6 (free base)

Synonym: Almogran; Almotrex; Amignul; Axert; Almotriptan Malate.

IUPAC/Chemical Name: N,N-dimethyl-2-(5-((pyrrolidin-1-ylsulfonyl)methyl)-1H-indol-3-yl)ethan-1-amine 2-hydroxysuccinate

InChi Key: QHATUKWEVNMHRY-UHFFFAOYSA-N

InChi Code: InChI=1S/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)

SMILES Code: CN(CCC1=CNC2=C1C=C(CS(=O)(N3CCCC3)=O)C=C2)C.O=C(O)C(O)CC(O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Related: 181183-52-8 (Almotriptan free base) 154323-57-6 (Almotriptan HCl)

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 335.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Almotriptan. 2021 May 17. PMID: 30000519.

2: Sidhu G, Preuss CV, Patel P. Almotriptan. 2022 Sep 21. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan–. PMID: 31082136.

3: Drugs for Migraine. Med Lett Drugs Ther. 2020 Oct 5;62(1608):153-160. PMID: 33434187.

4: Balbisi EA. Efficacy and safety of almotriptan malate for migraine. Am J Health Syst Pharm. 2002 Nov 15;59(22):2184-93. doi: 10.1093/ajhp/59.22.2184. PMID: 12455302.

5: Maasumi K, Tepper SJ, Kriegler JS. Menstrual Migraine and Treatment Options: Review. Headache. 2017 Feb;57(2):194-208. doi: 10.1111/head.12978. Epub 2016 Dec 2. PMID: 27910087.

6: Becker WJ. Acute Migraine Treatment in Adults. Headache. 2015 Jun;55(6):778-93. doi: 10.1111/head.12550. Epub 2015 Apr 15. PMID: 25877672.

7: Marmura MJ, Silberstein SD, Schwedt TJ. The acute treatment of migraine in adults: the american headache society evidence assessment of migraine pharmacotherapies. Headache. 2015 Jan;55(1):3-20. doi: 10.1111/head.12499. PMID: 25600718.

8: Singh RBH, VanderPluym JH, Morrow AS, Urtecho M, Nayfeh T, Roldan VDT, Farah MH, Hasan B, Saadi S, Shah S, Abd-Rabu R, Daraz L, Prokop LJ, Murad MH, Wang Z. Acute Treatments for Episodic Migraine [Internet]. Rockville (MD): Agency for Healthcare Research and Quality (US); 2020 Dec. Report No.: 21-EHC009. PMID: 33411427.

9: Keam SJ, Goa KL, Figgitt DP. Almotriptan: a review of its use in migraine. Drugs. 2002;62(2):387-414. doi: 10.2165/00003495-200262020-00010. PMID: 11817980.

10: Keam SJ, Goa KL, Figgitt DP. Spotlight on almotriptan in migraine. CNS Drugs. 2002;16(7):501-7. doi: 10.2165/00023210-200216070-00006. PMID: 12056924.

11: Gupta S, Perla A, Roy A, Vitore JG, K B, Salave S, Rana D, Sharma A, Rathod R, Kumar H, Benival D. In Vivo Evaluation of Almotriptan malate Formulation through Intranasal Route for the Treatment of Migraine: Systematic Development and Pharmacokinetic Assessment. AAPS PharmSciTech. 2023 Jan 10;24(1):32. doi: 10.1208/s12249-022-02496-2. PMID: 36627414.

12: McEnroe JD, Fleishaker JC. Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine. Clin Pharmacokinet. 2005;44(3):237-46. doi: 10.2165/00003088-200544030-00002. PMID: 15762767.

13: Pascual J. Almotriptan: an effective and well-tolerated treatment for migraine pain. Drugs Today (Barc). 2003;39 Suppl D:31-6. PMID: 15071618.

14: Ravikumar K, Sridhar B, Krishnan H, Singh AN. Almotriptan, an antimigraine agent, and its malate salt. Acta Crystallogr C. 2008 Jan;64(Pt 1):o15-7. doi: 10.1107/S0108270107060507. Epub 2007 Dec 14. PMID: 18216450.

15: Dowson AJ. Oral almotriptan: practical uses in the acute treatment of migraine. Expert Rev Neurother. 2004 May;4(3):339-48. doi: 10.1586/14737175.4.3.339. PMID: 15853532.

16: Pascual J, Vila C. Almotriptan: a review of 20 years' clinical experience. Expert Rev Neurother. 2019 Aug;19(8):759-768. doi: 10.1080/14737175.2019.1591951. Epub 2019 Mar 21. PMID: 30845850.

17: Pascual J, Vila C, McGown CC. Almotriptan: a review of 10 years' clinical experience. Expert Rev Neurother. 2010 Oct;10(10):1505-17. doi: 10.1586/ern.10.131. PMID: 20945537.

18: Mathew NT. Efficacy and tolerability of almotriptan in controlled clinical trials. Eur Neurol. 2005;53 Suppl 1:29-33. doi: 10.1159/000085039. Epub 2005 May 3. PMID: 15920335.

19: Bussone G, Allais G, Castagnoli Gabellari I, Benedetto C. Almotriptan for menstrually related migraine. Expert Opin Pharmacother. 2011 Aug;12(12):1933-43. doi: 10.1517/14656566.2011.594794. Epub 2011 Jul 5. PMID: 21726161.

20: Von S. Almotriptan: a review of pharmacology, clinical efficacy, and tolerability. Am J Manag Care. 2002 Feb;8(3 Suppl):S74-9. PMID: 11859907.

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