Dihydroergotoxine mesylate  (Synonyms: Ergoloid mesylates)

Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABA_A receptor associated Cl^- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity^{[1][2][3][4][5][6][7][8][9]}.Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABA_A receptor associated Cl^- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity^{[1][2][3][4][5][6][7][8][9]}.

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-K_m 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 (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

8067-24-1

Solid

White to off-white

[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

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

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

• [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]