An agonist of 5-HT1B and 5-HT1D receptors
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Almotriptan (malate)

Item No. 25646

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-hydroxy-butanedioic acid, compd. with N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-indole-3-ethanamine
CAS Number
181183-52-8
Synonyms
  • PNU 180638E
Molecular Formula
C17H25N3O2S • C4H6O5
Formula Weight
469.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.2 mg/mlDMSO: 0.1 mg/mlPBS (pH 7.2): 20 mg/ml
λmax
229 nm
SMILES
CN(C)CCC1=CNC2=CC=C(CS(N3CCCC3)(=O)=O)C=C21.OC(C(O)=O)CC(O)=O
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)
InChi Key
QHATUKWEVNMHRY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $42

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    10 mg

    $79

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    25 mg

    $183

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    50 mg

    $343

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    Product Description

    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).1 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.2 Formulations containing almotriptan have been used in the treatment of migraine headaches.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bou, J., Domènech, T., Puig, J., et al. Pharmacological characterization of almotriptan: An indolic 5-HT receptor agonist for the treatment of migraine. Eur. J. Pharmacol. 410(1), 33-41 (2000).

    2. Gras, J., Bou, J., Llenas, J., et al. Functional profile of almotriptan in animal models predictive of antimigraine activity. Eur. J. Pharmacol. 410(1), 43-51 (2000).