"目录号: HY-15310
Anti-infectionAutophagy-
Ivermectin是广泛使用于人类和动物的抗寄生虫剂。它是P2X4和α7nAChRs的正异构效应物。
ParasiteAutophagy
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生物活性
Description
Ivermectin is a widely used antiparasitic agent in human and veterinary medicine. It is a positive allosteric effector ofP2X4and the α7 neuronal nicotinic acetylcholine receptor (nAChRs).
In Vitro
Ivermectin (IVM) is a specific positive allosteric effector of heterologously expressed P2X4and possibly of heteromeric P2X4/ P2X6channels. In the submicromolar range (EC50=250 nM) the action of IVM is rapid and reversible, resulting in increased amplitude and slowed deactivation of P2X4channel currents evoked by ATP. IVM also markedly increases the potency of ATP and that of the normally low-potency agonist a,b-methylene-ATP in a use- and voltage-independent manner without changing the ion selectivity of P2X4channels[1]. IVM activates glutamate-gated chloride channels in the nerves and muscles of the parasite, leading to membrane hyperpolarization and muscle paralysis. The major mode of action of IVM is most likely the disruption of ingestive activity of the parasite, resulting in starvation[2]. Preapplication of ivermectin, in the micromolar range, strongly enhances the subsequent acetylcholine-evoked current of the neuronal chick or human α7 nicotinic acetylcholine receptors reconstituted in Xenopus laevis oocytes and K-28 cells[3]. Ivermectin activates the rat recombinant α1β2γ2sGABAAreceptor. Activation of the channel with 10 mM GABA results in currents rising within 1 ms to their maximal amplitudes. The EC50value for GABA is 7.5 μM[4].
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