| Bioactivity | Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease[1][2]. | ||||||||||||
| Target | α1A-adrenoceptor | ||||||||||||
| Invitro | Nicergoline (0.3-30 μM; 24 h) attenuates activated microglia- and astrocytes-induced neuronal cell death[3].Nicergoline (0.3-30 μM; 48 h) suppresses the production of proinflammatory cytokines and superoxide anion by activated microglia[3]. | ||||||||||||
| In Vivo | Nicergoline (10 mg/kg; i.v. once daily for 60 d) improves impaired neurogenesis and cognitive competence in mice with Alzheimer's disease[2].Nicergoline (10 mg/kg; i.v. once daily for 60 d) inhibits apoptosis, inflammation and oxidative stress in hippocampal cells, and regulates the activity of hippocampal cells through the PI3K/AKT signaling pathway in mice[2]. Animal Model: | ||||||||||||
| Name | Nicergoline | ||||||||||||
| CAS | 27848-84-6 | ||||||||||||
| Formula | C24H26BrN3O3 | ||||||||||||
| Molar Mass | 484.39 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Alvarez-Guerra, M., N. Bertholom, and R.P. Garay, Selective blockade by nicergoline of vascular responses elicited by stimulation of alpha 1A-adrenoceptor subtype in the rat. Fundam Clin Pharmacol, 1999. 13(1): p. 50-8. [2]. Zang G, et, al. Ameliorative effect of nicergoline on cognitive function through the PI3K/AKT signaling pathway in mouse models of Alzheimer's disease. Mol Med Rep. 2018 May;17(5):7293-7300. [3]. Mizuno T, et, al. Protective effects of nicergoline against neuronal cell death induced by activated microglia and astrocytes. Brain Res. 2005 Dec 20;1066(1-2):78-85. |