Dihydroergotoxine (mesylate)

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]}. 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-K_m 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].