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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
ZSET1446 is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models.
In Vitro
ZSET1446 (100 pM-10 nM) exerts limited effects on the basal neuronal excitability and synaptic transmission. ZSET1446 potentiates the facilitatory effect of nAChR stimulation on sPSC frequency. ZSET1446 potentiates the increase in sIPSC frequency by local application of nicotine (5 µM; 2 minutes) without affecting the basal sIPSC frequency at the range of 10 pM to 1 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ZSET1446 enhances object recognition memory in mice and ameliorates cognitive impairment caused by scopolamine in rats. Concomitant administration of subeffective doses of ZSET1446 and memantine significantly ameliorates the cognitive performance in the novel object recognition task in both mice and rats. Moreover, oral administration of ZSET1446 or memantine increases the extracellular level of ACh in the hippocampus as compared with the control. Further, concomitant administration of subeffective doses of ZSET1446 and memantine significantly increases the extracellular level of ACh as compared with the group of ZSET1446 or memantine alone. ZSET1446 (0.002, 0.01, and 0.1 mg/kg, p.o.) ameliorates cognitive deficits of SAMP8 after 4, 8, 12, and 16 weeks of treatment in a novel object recognition test. ZSET1446 also reduces grading scores of SAMP8 after 16 weeks of treatment. Further, 8-week treatment of ZSET1446 significantly reduces the total number of Aβ-positive granules in the hippocampus. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
The experimental apparatus consists of a Plexiglas open-field box [25 cm (width) × 41 cm (length) × 17 cm (depth), model TP-105], the floor of which is covered with sawdust. The apparatus is located in a sound-attenuated room. The procedure for the novel object recognition task consists of three different sessions: habituation, training, and retention sessions. Each mouse is individually habituated to the box, with 10 min of exploration in the absence of objects (day 1: habituation session). ZSET1446 at doses of 0.001, 0.003, 0.01, and 0.03 mg/kg and/or memantine at doses of 3 and 10 mg/kg is orally administered 60 min before the training trial. In the experiment of injection of nicotinic receptor antagonists, oral administration of ZSET1446 and i.p. injection of mechamylamine or DHbE at each dose of 1 mg/kg are given 60 min before the training trial. During the training session, two different novel objects are symmetrically fixed to the floor in the box, and each animal is allowed to explore in the box for 10 min (day 2: training session). These objects are different in shape and color but similar in size. The mice are considered to be exploring the object when the mouse is facing, touching, or sniffing the object. The time spent for exploring each object is manuallymeasured by a stopwatch. In the training session, locomotor activity is simultaneously measured for a period of 10 min automatically, using an Animex Auto placed under the open-field box. After the training trial, mice are immediately returned to their home cages. aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
分类树(Taxonomy Tree)
| 界(kingdom) | 有机化合物 |
|---|---|
| 超类(Superclass) | 有机杂环化合物 |
| 类(Class) | 咪唑并吡啶类 |
| 亚类(Subclass) | 咪唑并吡啶酮 |
| 中间层级节点(Intermediate Tree Nodes) | 暂无 |
| 直接上位类(Direct Parent) | 咪唑并吡啶酮 |
| 其他上位类(Alternative Parents) | α氨基酸及其衍生物 Indanes 吡啶酮类 二氢吡啶 咪唑啉酮类 N-酰亚胺 炔丙基型1,3-偶极有机化合物 烯胺 甲脒类 甲脒类 氮杂环化合物 有机氧化物 碳氢化合物衍生物 羰基化合物 |
| 分子骨架(Molecular Framework) | 芳香族杂多环化合物 |
| 取代基(Substituents) | 2-碘苯酚 - α-氨基酸或其衍生物 - 氨基脒 - 氨基酸 - 芳香族杂多环化合物 - 氮杂环 - 苯基化合物 - 羰基 - 羧酰亚胺 - 羧酰胺基 - 羧酸衍生物 - 二氢吡啶 - 萘醌 - 烃衍生物 - 咪唑啉酮 - 咪唑哌啶酮 - 茚烷 - N-酰基亚胺 - 有机1,3-双极性化合物 - 有机硝基化合物 - 有机氧化物 - 有机氧化合物 - 有机氮化合物 - 有机氧化合物 - 丙炔型1,3-双极性有机化合物 - 吡啶酮 |
| 描述(Description) | 该化合物属于有机化合物中的咪唑吡啶酮类。这类化合物含有咪唑吡啶结构单元,其中吡啶环上带有酮基团。 |
| 外部描述符(External Descriptors) | 暂无 |