Dihydroergotamine mesylate

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

6190-39-2

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	White solid
Storage	Store at -20°C
M.Wt	679.78
Cas No.	6190-39-2
Formula	C₃₄H₄₁N₅O₈S
Solubility	insoluble 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)
Canonical SMILES	C[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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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-HT_1Band 5-HT_1Dreceptors 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-HT_1Band 5-HT_1Dreceptors 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.

试验操作

Cell experiment:[2]
Cell lines	LMTK- cells expressing 5-HT_2Bor 5-HT_2Creceptors
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-HT_2Band 7.83 ± 0.06 at 5-HT_2Creceptors.
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 D₂dopaminergic 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-HT_1Band 5-HT_1Dreceptors 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.