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Dihydroergotamine mesylate

Catalog No.
B3459
An ergot derivative with agonistic activity for α-adrenergic, dopaminergic, and serotonergic receptors
Grouped product items
SizePriceStock Qty
10mg
$59.00
Ship with 10-15 days
50mg
$132.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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.?

References:

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.

Chemical Properties

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt679.78
Cas No.6190-39-2
FormulaC34H41N5O8S
Solubilityinsoluble in EtOH; ≥102.2 mg/mL in DMSO; ≥2.85 mg/mL in H2O with gentle warming and ultrasonic
Chemical 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)
SDFDownload SDF
Canonical SMILESC[C@@](/N=C(O)/[C@](C1)([H])C[C@]2([H])C3=C4C(C[C@@]2([H])N1C)=CNC4=CC=C3)(O5)C(N([C@]5(O)[C@]6([H])CCCN67)[C@@](C7=O)([H])CC8=CC=CC=C8)=O.CS(O)(=O)=O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment:[2]

Cell lines

LMTK- cells expressing 5-HT2B or 5-HT2C receptors

Reaction Conditions

30 min incubation

Applications

Dihydroergotamine (DHE) and its major metabolite 8'-hydroxy-DHE (8'-OH-DHE) acted as agonists for both 5-HT2B and 5-HT2C receptors in respect to cGMP production, with pEC50 values of 8.32 ± 0.09 for 8'-OH-DHE at 5-HT2B and 7.83 ± 0.06 at 5-HT2C receptors.
Animal experiment:[3]

Animal models

Anaesthetized Yorkshire pigs

Dosage form

3, 10, 30 and 100 mg/kg

i.v.

Applications

Dihydroergotamine mesylate elicited dose-dependent pressor and bradycardic responses which were probably mediated by its partial agonist action on α-adrenoceptors and D2 dopaminergic receptors. The carotid haemodynamic effects of dihydroergotamine mesylate consisted of a dose-dependent reduction of arteriovenous anastomotic blood flow and conductance and an increase in nutrient (tissue) blood flow and conductance.

Note

The technical data provided above is for reference only
?

References:

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.