| 货号 | 19547-1mg |
| 描述 | Linopirdine is an enhancer of the stimulus-evoked but not basal release of several neurotransmitters, including acetylcholine, dopamine, serotonin, and glutamate. It increases acetylcholine release in rat hippocampal CA1 neurons by blocking voltage-gated, calcium-activated and leak (M-type; Kv7.2/7.3; KCNQ2/3) K+ current with an IC50 value of 2.4 µM.1,2 Inhibition of M-channels is reported to result in the depolarization of CA3 pyramidal neurons and activated presynaptic voltage-gated P/Q- and N-type calcium channels, which leads to Ca2+ influx and increased neurotransmitter release.3 Linopirdine has been shown to produce a number of effects including EEG patterns of enhanced vigilance, induction of c-fos expression in cerebral cortex, reduction of the increase of cerebral glucose utilization induced by hypoxia, and improved performance in animal models of learning and memory.4 Linopirdine has also been identified as an agonist of transient receptor potential vanilloid type 1 (EC50 = 115 µM in HEK293 cells voltage clamped at -60 mV).5 |
| 别名 | DuP-996; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Schnee, M.E., and Brown, B.S. Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. Journal of Pharmacology and Experimental Therapeutics 286(2), 709-717 (1998). 2.Kristufek, D.,Koth, G.,Motejlek, A., et al. Modulation of spontaneous and stimulation-evoked transmitter release from rat sympathetic neurons by the cognition enhancer linopirdine: Insights into its mechanisms of action. Journal of Neurochemistry 72(50), 2083-2091 (1999). 3.Sun, J., and Kapur, J. M-type potassium channels modulate Schaffer collateral-CA1 glutamatergic synaptic transmission. Journal of Physiology 590(16), 3953-3964 (2012). 4.Tam, S.W., and Zaczek, R. Linopirdine. A depolarization-activated releaser of transmitters for treatment of dementia. Advances in Experimental Medicine and Biology 363, 47-56 (1995). 5.Neacsu, C., and Babes, A. The M-channel blocker linopirdine is an agonist of the capsaicin receptor TRPV1. Journal of Pharmacological Sciences 114(3), 332-340 (2010). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 464.4 |
| 分子式 | C26H21N3O • 2HCl |
| CAS号 | 113168-57-3 |
| 稳定性 | ≥ 2 years |
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