Veralipride是D2受体的拮抗剂。它是一种替代抗抑郁药治疗绝经期症状的药物。
CAS：66644-81-3
分子式：C17H25N3O5S
分子量：383.46
纯度：98%
存储：Store at -20°C

Background:

Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms.

Veralipride administration (100 mg/day for 30 days) induces a significant reduction in vasomotor symptoms and is more effective than placebo. Treatment is followed by the expected increase in plasma prolactin levels and by a significant decrease in mean plasma LH. A significant reduction is observed in objectively recorded hot flushes after Veralipride treatment[1]. Veralipride is well absorbed when administered orally, achieving maximal concentrations at 2.5 hours. It is poorly metabolized and is eliminated in the urine and feces. After oral administration, the half-life is 4 hours, and 44% is excreted without any changes in urine in the first 120 hours[2]. A total of 57 adverse events are registered during the 386-month treatment. For the 20×10 dosing schedule, the highest incidence is observed for anxiety (2.2%), drowsiness, and weakness (1.5%); for the 5 × 2 dosing schedule, the highest incidence is observed for drowsiness (5.3%) and headache (2.6%)[3]. Veralipride is known to cause extrapiramidal signs such as bucco-facial or limb dyskinesia. Veralipride may cause reversible parkinsonism[4].

[1]. Melis GB, et al. Effects of the dopamine antagonist veralipride on hot flushes and luteinizing hormone secretion in postmenopausal women. Obstet Gynecol. 1988 Nov;72(5):688-92. [2]. Carranza-Lira S, et al. Actual status of veralipride use. Clin Interv Aging. 2010 Sep 7;5:271-6. [3]. Valencia MH, e al. Safety of veralipride for the treatment of vasomotor symptoms of menopause. Menopause. 2014 May;21(5):484-92. [4]. Franchignoni FP, et al. Parkinson syndrome induced by veralipride. Minerva Ginecol. 1995 Jun;47(6):277-9.