An agonist of 5-HT1B and 5-HT1D receptors
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Metabolite(s)
34302N-desmethyl Eletriptan
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Eletriptan

Item No. 20048

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[(2R)-1-methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole
CAS Number
143322-58-1
Synonyms
  • UK 116044
Molecular Formula
C22H26N2O2S
Formula Weight
382.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/mlEthanol: 0.1 mg/ml
λmax
223, 271 nm
SMILES
CN(CCC1)[C@H]1CC2=CNC3=CC=C(CCS(C4=CC=CC=C4)(=O)=O)C=C32
InChi Code
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
InChi Key
PWVXXGRKLHYWKM-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

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    Product Description

    Eletriptan is an agonist of the serotonin (5-HT) receptor types 5-HT1B and 5-HT1D.1 It inhibits forskolin-induced cAMP accumulation in and induces vasoconstriction of isolated rabbit common carotid artery rings (pD2s = 7.6 and 4.9, respectively), an effect that can be blocked by the 5-HT1B antagonist SB216641 but not the 5-HT1D antagonist BRL15572. Eletriptan preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively).2 Formulations containing eletriptan have been used in the treatment of migraine headache.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Akin, D., Onaran, H.O., and Gudal, H. Agonist-directed trafficking explaining the difference between response pattern of naratriptan and sumatriptan in rabbit common carotid artery. Br. J. Pharmacol. 136(2), 171-176 (2002).

    2. Edvinsson, L., Uddman, E., Wackenfors, A., et al. Triptan-induced contractile (5-HT1B receptor) responses in human cerebral and coronary arteries: Relationship to clinical effect. Clin. Sci. (Lond.) 109(3), 335-342 (2005).