Eletriptan - CAS 143322-58-1
Catalog number: 143322-58-1
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C₂₂H₂₆N₂O₂S
Molecular Weight:
382.52
COA:
Inquire
Targets:
5-HT Receptor
Description:
Eletriptan is Serotonin 1D receptor agonist originated by Pfizer. It is a second generation triptan drug. It is used as an abortive medication, blocking a migraine attack which is already in progress. Eletriptan was approved by the FDA for the acute treatment of migraine with or without aura in adults in 2002.
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Purity:
98%
Appearance:
Yellow to Dark Yellow Solid
Synonyms:
3-[[(2R)-1-Methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole; (R)-5-[2-(Benzenesulfonyl)ethyl]-3-[(N-methylpyrrolidin-2-yl)methyl]-1H-indole; UK-116044; Relpax free amine;
Solubility:
Chloroform (Slightly), Methanol (Slightly)
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Menstrual migraine; Migraine
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
No Data Available
Melting Point:
46-48°C
InChIKey:
PWVXXGRKLHYWKM-LJQANCHMSA-N
InChI:
1S/C22H26N2O2S/c1-24-12-5-6-19(24)15-18-16-23-22-10-9-17(14-21(18)22)11-13-27(25,26)20-7-3-2-4-8-20/h2-4,7-10,14,16,19,23H,5-6,11-13,15H2,1H3/t19-/m1/s1
Canonical SMILES:
CN1CCC[C@@H]1Cc2c[nH]c3c2cc(cc3)CCS(=O)(=O)c4ccccc4
Current Developer:
Originator Pfizer
1.A review of the pharmacoeconomics of eletriptan for the acute treatment of migraine.
Bhambri R1, Mardekian J1, Liu LZ2, Schweizer E3, Ramos E1. Int J Gen Med. 2015 Jan 12;8:27-36. doi: 10.2147/IJGM.S73673. eCollection 2015.
Migraine is a commonly occurring, chronic disorder that can cause significant disability. Eletriptan, a selective serotonin 5-hydroxytryptamine 1 receptor subtype B/D (5-HT1B/1D) agonist, is a clinically effective treatment for moderate to severe migraine. The objective of this literature review was to summarize the available data on the pharmacoeconomics of eletriptan relative to other triptans. Articles meeting the following three criteria were included in the review: 1) contained pharmacoeconomic data on a marketed dose of eletriptan; 2) included data on at least one other comparator triptan; and 3) was in English. A MEDLINE(®) search yielded a total of eight studies (from the European Union [n=5] and from the USA [n=3]) across multiple regions. Seven of the studies examined the pharmacoeconomics of eletriptan relative to other triptans, and a further study examined the health care costs of eletriptan 40 mg versus sumatriptan 100 mg. Eletriptan 40 mg was among a group of triptans, including rizatriptan 10 mg and almotriptan 12.
2.Thermoreversible nanoethosomal gel for the intranasal delivery of Eletriptan hydrobromide.
Shelke S1, Shahi S2, Jadhav K3, Dhamecha D3, Tiwari R4, Patil H4. J Mater Sci Mater Med. 2016 Jun;27(6):103. doi: 10.1007/s10856-016-5713-6. Epub 2016 Apr 18.
The objective of the current study was to formulate and characterize thermoreversible gel of Eletriptan Hydrobromide for brain targeting via the intranasal route. Ethosomes were prepared by 3(2) factorial design with two independent variables (concentration of soya lecithin and ethanol) and two response variables [percent entrapment efficiency and vesicle size (nm)] using ethanol injection method. Formulated ethosomes were evaluated for preliminary microscopic examination followed by percent drug entrapment efficiency, vesicle size analysis, zeta potential, polydispersibility index and Transmission electron microscopy (TEM). TEM confirms spherical morphology of ethosomes, whereas Malvern zeta sizer confirms that the vesicle size was in the range of 191 ± 6.55-381.3 ± 61.0 nm. Ethosomes were incorporated in gel using poloxamer 407 and carbopol 934 as thermoreversible and mucoadhesive polymers, respectively. Ethosomal gels were evaluated for their pH, viscosity, mucoadhesive strength, in vitro drug release and ex vivo drug permeation through the sheep nasal mucosa.
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CAS 143322-58-1 Eletriptan

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