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Dihydroergotoxine mesylate

MCE China：Dihydroergotoxine mesylate

Brand：MedChemExpress (MCE)

Cat. No.HY-B0799

CAS：8067-24-1

Synonyms：Ergoloid mesylates

Purity：99.88%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：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].

In Vivo：Dihydroergotoxine mesylate (30 mg/kg, i.p.) prevents delayed neuronal death (CA1) in the gerbil hippocampus[5]. 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].

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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]