Dihydroergotamine mesylate

Dihydroergotamine mesylate

Catalog Number:
L002370527APE
Mfr. No.:
APE-B3459
Price:
$194
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          Background

          Dihydroergotamine mesylate is a partial agonist for both dopaminergic and α-adrenergic receptors. Dihydroergotamine mesylate also acts as a full agonist for the 5-HT receptor, with IC50 values being 2 nM and 2.2 nM for human 5-HT1B and 5-HT1D receptors stably expressed in HEK 293 cells and C6 glioma cells, respectively. Like other potent 5-HT receptor agonists such as sumatriptan, dihydroergotamine mesylate has been approved for acute migraine therapy.

          1. Lesage AS, Wouters R, Van Gompel P, et al. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. British Journal of Pharmacology, 1998, 123(8): 1655-1665.
          2. Schaerlinger B, Hickel P, Etienne N, et al. Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy. British Journal of Pharmacology, 2003, 140(2): 277-284.
          3. Villalón CM, Bom AH, Den Boer MO, et al. Effects of S9977 and dihydroergotamine in an animal experimental model for migraine. Pharmacological Research, 1992, 25(2): 125-137.

      • Properties
        • Categories
          An ergot derivative with agonistic activity for α-adrenergic, dopaminergic, and serotonergic receptors
          Alternative Name
          (6aR,9R,10aR,Z)-N-((2R,5S,10aS,10bS)-5-benzyl-10b-hydroxy-2-methyl-3,6-dioxooctahydro-2H-oxazolo[3,2-a]pyrrolo[2,1-c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carbimidic acid compound with methanesulfonic acid (1:1)
          CAS Number
          6190-39-2
          Molecular Formula
          C34H41N5O8S
          Molecular Weight
          679.78
          Appearance
          White solid
          Solubility
          insoluble in EtOH; ≥102.2 mg/mL in DMSO; ≥2.85 mg/mL in H2O with gentle warming and ultrasonic
          Storage
          Store at -20°C
          SMILES
          C[[email protected]@](/N=C(O)/[[email protected]](C1)([H])C[[email protected]]2([H])C3=C4C(C[[email protected]@]2([H])N1C)=CNC4=CC=C3)(O5)C(N([[email protected]]5(O)[[email protected]]6([H])CCCN67)[[email protected]@](C7=O)([H])CC8=CC=CC=C8)=O.CS(O)(=O)=O

          * For Research Use Only

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