Dihydroergotoxine mesylate  (Synonyms: 甲磺酸二氢麦角碱; 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) 可抑制人前列腺癌细胞 (LNCaP、MDA-PCA-2b、DU145 和 PC3) 的增殖，在 12 和 25 μg/mL 之间 (18–38 μM) 可观察到半数最大生长抑制作用^[3]。
Dihydroergotoxine mesylate (5.5-88 μM, 10 min) 在猫和大鼠脑匀浆中对低 K_m 磷酸二酯酶 (PE) 的抑制作用强于对高 K_m 磷酸二酯酶 (PE) 的抑制作用^[7]。

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

Dihydroergotoxine mesylate (30 mg/kg，腹腔注射) 可防止沙鼠海马神经元延迟死亡 (CA1) ^[5]。
Dihydroergotoxine mesylate (0.08 mg/kg，灌注，20 min) 对脑代谢紊乱具有保护作用 (猫的脑电图活动趋于稳定，pO₂ 分布向正常张力状态方向移动)^[6]。
Dihydroergotoxine mesylate (3 mg/kg，腹腔注射) 可改变大鼠的睡眠-觉醒周期，增加觉醒，减少慢波睡眠和快速眼动睡眠^[8]。
Dihydroergotoxine (10 μg/kg，皮下注射) mesylate 通过与外周多巴胺受体相互作用降低自发性高血压大鼠的血压^[9]。

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

8067-24-1

固体

White to off-white

甲磺酸双氢麦角碱；甲磺酸二氢麦角碱

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]