Zaleplon, indiplon, and eszopiclone modulate γ3-containing GABA A receptors at therapeutically relevant doses while diazepam, zolpidem, and alpidem do not. On α1β2γ3 receptors, zaleplon has equal efficacy compared with α1β2γ2, and a four-fold increase in potency.

2023年6月21日 · Zaleplon, a pyrazolopyrimidine hypnotic, binds to the benzodiazepine type 1 site on the gamma-aminobutyric acid subtype A (GABA-A) receptor/chloride-ion channel complex. The chemical name of zaleplon, is N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7 …

扎来普隆（Zaleplon），是一种有机化合物，化学式为C17H15N5O，呈淡黄色结晶粉末。 扎来普隆为镇静催眠药，临床上主要用于失眠的短时间的治疗，可以使失眠病人很快入睡，缩短入睡时间，延长睡眠时间，减少觉醒的次数，被列为第二类精神药品管控。

2023年12月12日 · Our results, showing that zaleplon enhances GABA neurotransmission in the hippocampus, were not surprising. However, we found that treatment also increased glutamatergic signaling. This could be the result of the downregulation of adenosine A1 receptors, important modulators of the glutamatergic system.

Zaleplon, zolpidem and zopiclone are structurally distinct. Due to variation in binding to the GABA receptor subunits, these three compounds show subtle differences in their effect on sleep stages, and as antiepileptics, anxiolytics and amnestics.

2002年9月13日 · The modulatory action of zaleplon at GABA A receptors has now been compared with those of zolpidem and the triazolobenzodiazepine triazolam. Zaleplon potentiated GABA-evoked Cl − currents in Xenopus oocytes expressing human GABA A receptor subunits with a potency that was higher at α1β2γ2 receptors than at α2- or α3-containing receptors.

2020年11月19日 · In this study, we evaluated the modulatory properties of five non-benzodiazepine Z-drugs (zaleplon, indiplon, eszopiclone, zolpidem, and alpidem) used in sleep management and the benzodiazepine, diazepam on human α1β2γ …

2002年9月13日 · The modulatory action of zaleplon at GABA(A) receptors has now been compared with those of zolpidem and the triazolobenzodiazepine triazolam. Zaleplon potentiated GABA-evoked Cl(-) currents in Xenopus oocytes expressing human GABA(A) receptor subunits with a potency that was higher at alpha1beta2gamma2 receptors than at alpha2- or alpha3 ...

non-benzodiazepine Z-drugs (zaleplon, indiplon, eszopiclone, zolpidem, and alpidem) used in sleep management and the benzodiazepine, diazepam on human a1b2g receptors using all three g subtypes. This was accomplished using concatenated GABAA pentamers expressed in Xenopus laevis oocytes and measured via two-electrode voltage clamp.

2020年11月1日 · In this study, we evaluated the modulatory properties of five non-benzodiazepine Z-drugs (zaleplon, indiplon, eszopiclone, zolpidem, and alpidem) used in sleep management and the benzodiazepine,...