Dihydroergotoxine mesylate
Based on 1 Customer Validation
Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABAA receptor associated Cl- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity.Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABAA receptor associated Cl- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity.
For research use only. We do not sell to patients.
- Purity: 99.61%
- CAS No.: 8067-24-1
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Biological Activity
Dihydroergotoxine mesylate (0-50 μg/mL) inhibits the proliferation of human prostate cancer cell lines (LNCaP, MDA-PCA-2b, DU145 and PC3), with half-maximal growth-inhibition observed between 12 and 25 μg/mL (18–38 μM)[3].
Dihydroergotoxine mesylate (5.5-88 μM, 10 min) is shown to be a stronger inhibitor of the low-Km than of the high-Km phosphodiesterase (PE) in cat and rat brain homogenates[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Dihydroergotoxine mesylate (0.08 mg/kg, infused, 20 min) exerts a protective effect on the oligemically disturbed brain metabolism (stabilization of EEG activity and shift of pO2 distribution in direction of normotonic state in cats[6].
Dihydroergotoxine mesylate (3 mg/kg, i.p.) alters the sleep-wakefulness cycle of the rat by increasing wakefulness and decreasing slow wave and rapid eye movement sleep[8].
Dihydroergotoxine (10 μg/kg s.c.) mesylate decreases blood pressure in spontaneously hypertensive rats by interacting with peripheral dopamine receptors[9].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 8067-24-1
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Appearance Solid
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Color White to off-white
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SMILES
[H][C@]1([C@]2([H])C[C@@H](C(N[C@@]3(C(C)C)C(N([C@@H]([R])C(N4[C@@]5([H])CCC4)=O)[C@@]5(O)O3)=O)=O)CN1C)CC6=CNC7=C6C2=CC=C7.CCC8=CC=CC=C8.CC(C)C.CC(CC)C.CC(C)CC.OS(=O)(C)=O
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Synonyms
Ergoloid mesylates
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 175 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Tvrdeic A, et al. Dihydrogenated ergot compounds bind with high affinity to GABAA receptor-associated Cl- ionophore. Eur J Pharmacol. 1991 Sep 4;202(1):109-11. [Content Brief]
[2]. Tvrdeic A, et al. Effect of ergot alkaloids on 3H-flunitrazepam binding to mouse brain GABAA receptors. Coll Antropol. 2003;27 Suppl 1:175-82. [Content Brief]
[3]. Abdul M, et al. Expression of gamma-aminobutyric acid receptor (subtype A) in prostate cancer. Acta Oncol. 2008;47(8):1546-50. [Content Brief]
[4]. Cheng YQ, Ge NN, Zhu HH, Sha ZT, Jiang T, Zhang YD, Tian YY. Dihydroergotoxine mesylate for the treatment of sialorrhea in Parkinson's disease. Parkinsonism Relat Disord. 2019 Jan;58:70-73. [Content Brief]
[5]. Izumiyama K, Kogure K. Effect of dihydroergotoxine mesylate (Hydergine) on delayed neuronal death in the gerbil hippocampus. Acta Neurol Scand. 1988 Sep;78(3):214-20. [Content Brief]
[6]. Gygax P, et al. Effect of papaverine and dihydroergotoxine mesylate on cerebral microflow, EEG, and pO2 in oligemic hypotension. Gerontology. 1978;24 Suppl 1:14-22. [Content Brief]
[7]. Enz A, et al. The influence of dihydroergotoxine mesylate on the low-Km phosphodiesterase of cat and rat brain in vitro. Gerontology. 1978;24 Suppl 1:115-25. [Content Brief]
[8]. Carruthers-Jones DI, et al. Changes in the rat electrocorticogram following administration of two dihydrogenated ergot derivatives. Gerontology. 1978;24 Suppl 1:23-33. [Content Brief]
[9]. Memo M, et al. Dihydroergotoxine decreases blood pressure in spontaneously hypertensive rats by interacting with peripheral dopamine receptors. Life Sci. 1985 Apr 22;36(16):1515-22. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dihydroergotoxine mesylate Related Classifications
HY-B0799 Related Classifications
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