2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein Stem Cell/Wnt MAPK/ERK Pathway Epigenetics
  3. nAChR 5-HT Receptor ERK Epigenetic Reader Domain
  4. A-582941

A-582941 是一种选择性的、口服有效的、可通过血脑屏障的 α7 nAChR 激动剂，对大鼠脑和人额叶皮层的 Ki 分别为 10.8 和 17 nM。A-582941 对 5-HT3 受体具有激动活性，其 Ki 为 150 nM。A-582941 可触发 ERK1/2 和 CREB 磷酸化，通过 Ser-9 磷酸化抑制 GSK-3β，增加乙酰胆碱释放，诱导 Arc 和 c-Fos 的表达，激活与工作记忆及注意力相关的脑区，并减少神经生长因子 (NGF) 剥夺导致的细胞死亡。A-582941 可用于阿尔茨海默病和精神分裂症的研究。

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A-582941

A-582941 Chemical Structure

CAS No. : 848591-89-9

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A-582941 的其他形式现货产品:

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A-582941 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia[1][2][3].

IC50 & Target[1]

5-HT3 Receptor

150 nM (Ki)

体外研究
(In Vitro)

A-582941 能以高亲和力结合大鼠脑 (Ki = 10.8 nM) 和人额叶皮层 (Ki = 17 nM) 细胞膜中的 α7 nAChRs，而对大鼠脑中经拮抗剂标记的 α7 nAChRs 的亲和力略低 (Ki = 88 nM)[1]。
A-582941 是爪蟾卵母细胞中重组人源 α7 nAChR 的部分激动剂，其 EC50 为 4260 nM，相对于乙酰胆碱的效能为 52%[1]。
A-582941 是爪蟾卵母细胞中重组大鼠 α7 nAChRs 的部分激动剂，其 EC50 为 2450 nM，相对于乙酰胆碱的效能为 60%[1]。
A-582941 (预先孵育 3 μM PNU-120596 后再给药) 在爪蟾卵母细胞中重组人源 α7 nAChR 上表现出增强的效力 (EC50 = 580 nM) 和效能 (相对于乙酰胆碱为 207%)[1]。
A-582941 可在表达 α7 nAChR 的 PC12 细胞中增强 ERK1/2 的磷酸化，其 EC50 为 95 nM，该效应由 α7 nAChRs 介导[1]。
A-582941 (0.1-100 μM) 可保护 PC12 细胞免受 NGF 撤除诱导的细胞死亡[1]。
A-582941 (100 nM-10,000 nM; 9 days) 不会诱导培养的人角质形成细胞增殖[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

A-582941 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Cultured human keratinocytes
Concentration: 100 nM, 10,000 nM
Incubation Time: 9 days, with medium refreshed every 3-4 days
Result: Produced no detectable proliferation under conditions where serum/growth factor supplements evoked significant proliferative events.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Vss CLplasma Cmax Bioavailability
Mice[1] 1.0 μmol/Kg i.v. 1.4 h 11.4 L/kg 7.9 L/h/kg / /
Mice[1] 1.0 μmol/Kg p.o. / / / 18 ng/mL ~100 %
Rat[1] 6.2 μmol/Kg i.v. 1.5 h 9.2 L/kg 4.7 L/h/kg / /
Rat[1] 6.2 μmol/Kg p.o. / / / 114 ng/mL 90 %
Dog[1] 0.5 μmol/Kg i.v. 1.4 h 7.9 L/kg 5.3 L/h/kg / /
Dog[1] 3.0 μmol/Kg p.o. / / / 79 ng/mL 22 %
Monkey[1] 0.5 μmol/Kg i.v. 2.0 h 3.9 L/kg 1.6 L/h/kg / /
Monkey[1] 3.0 μmol/Kg p.o. / / / 39 ng/mL 50 %
体内研究
(In Vivo)

A-582941 (0.01-1.00 μmol/kg；腹腔注射) 可呈剂量依赖性地增强与认知相关的小鼠脑区中 ERK1/2 和 CREB 的磷酸化水平[1]。
A-582941 (0.01-1.00 μmol/kg；腹腔注射) 可改善小鼠的记忆巩固，在 0.1 μmol/kg 时达到完全药效[1]。
A-582941 (0.1-1.0 μmol/kg；腹腔注射) 可剂量依赖性地增加小鼠扣带回皮层中 Ser-9 GSK-3β 的磷酸化水平[1]。
A-582941 (0.1-1.0 μmol/kg；腹腔注射) 可改善大鼠的短期识别记忆，在 0.1 μmol/kg 剂量下即可达到完全药效[1]。
A-582941 (3 μmol/kg；腹腔注射；每日 1 次；连续 3 天) 可适度增加自由活动大鼠内侧前额叶皮层的乙酰胆碱释放量[1]。
A-582941 (1.8 μmol/kg；皮下注射；持续输注；7 天) 在改善大鼠短期识别记忆方面维持疗效[1]。
A-582941 (0.003-0.100 μmol/kg；肌肉注射) 可改善幼年恒河猴的工作记忆，在 0.01 μmol/kg 剂量下即可达到完全药效[1]。
A-582941 (10 μmol/kg；腹腔注射) 可逆转大鼠中由 MLA (HY-N2332) 诱导的感觉门控缺陷[1]。
A-582941 (3-10 μmol/kg；腹腔注射) 可改善 DBA/2J 小鼠的遗传性感觉门控缺陷，连续 5 天给予 3 μmol/kg (腹腔注射) 给药后仍能保持药效[1]。
A-582941 (0.1-1.0 μmol/kg；皮下注射) 可轻度改善自发性高血压幼鼠的反应抑制/冲动行为[1]。
A-582941 (0.1-10 mg/kg；皮下注射；单次给药) 可在幼年雄性 Wistar 大鼠的边缘前脑区域诱导 Arc 和 c-Fos 的 mRNA 及蛋白表达呈剂量依赖性升高，其中 10 mg/kg 时效应达到最大，且幼年大鼠的反应性相较于成年大鼠更强[2]。
A-582941 (0.1-10 mg/kg；皮下注射；单次给药) 在 10 mg/kg 剂量下可增加成年雄性 Wistar 大鼠边缘前脑区的 Arc 和 c-Fos 免疫反应阳性细胞计数，但在所有检测区域中均未诱导 Arc 或 c-Fos mRNA 表达出现可检测到的升高[2]。
A-582941 (1.14-38 μg/kg；肌肉注射；单次给药) 可显著提升青年恒河猴的延迟样本匹配任务正确率，其长延迟试次的正确率提升 22.2%(为短延迟试次提升幅度的两倍)，但该提升效果在给药 24 小时后无法维持[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: unspecified strain[1]
Dosage: 1.8 μmol/kg/day
Administration: s.c.; continuous infusion; 7 days
Result: Maintained efficacy in the social recognition test, as reflected by a reduced ratio of investigative behavior during the second session (T2) compared to the first session (T1).
Reached a mean steady-state plasma concentration of 3.1 ± 0.3 ng/mL (11 nM).
Animal Model: DBA/2J[1]
Dosage: 3 μmol/kg (acute; 5-day repeated dosing); 10 μmol/kg (acute)
Administration: i.p.; acute; once daily; 5 consecutive days
Result: Significantly improved sensory gating in acutely treated mice.
Retained efficacy after 5 consecutive days of dosing with 3 μmol/kg (i.p.).
Reached an average plasma concentration of 44 ng/mL (157 nM) after 5 days of repeated dosing.
Animal Model: Wistar rats (adult, male, approximately 55 days, 210-230 g)[2]
Dosage: 0.1, 0.3, 1, 3 and 10 mg/kg
Administration: s.c.; single dose
Result: Did not induce significant increases in Arc or c-Fos mRNA expression in any brain region examined (mPFC, VO/LO cortex, hippocampus).
Increased Arc immunoreactive cell counts at 10 mg/kg in the mPFC (262% increase vs controls), VO/LO cortex (233% increase vs controls), ACCshell (851% increase vs controls), and dmSTR (419% increase vs controls); no significant effect was seen in the ACCcore or dlSTR.
Increased c-Fos immunoreactive cell counts at 10 mg/kg in the mPFC (97% increase vs controls), VO/LO cortex (115% increase vs controls), and ACCshell (169% increase vs controls); no significant effect was seen in the ACCcore, dmSTR, or dlSTR.
Animal Model: Macaca mulatta (male, 9-18 years old, 7.2-11.8 kg)[3]
Dosage: 1.14 μg/kg; 3.8 μg/kg; 11.4 μg/kg; 38 μg/kg
Administration: i.m.; single dose
Result: Significantly improved delayed matching-to-sample (DMTS) task accuracies relative to vehicle controls.
Produced a significant increase in short delay trial accuracy at 11.4 μg/kg dose.
Produced significant increases in long delay trial accuracy at 1.14 μg/kg, 3.8 μg/kg, and 11.4 μg/kg doses.
Increased long delay trial accuracy by 22.2% above control, approximately twice the 11.3% increase observed in short delay trials.
Showed a non-significant trend toward improved accuracy at 38 μg/kg dose.
Produced no statistically significant improvement in task accuracies during sessions initiated 24 hours after dosing, despite mean long delay accuracies remaining above vehicle levels.
Produced no significant effect on sample or choice task latencies.
分子量

280.38

Formula

C17H20N4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

A-582941 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

A-582941848591-89-9A582941A 582941nAChR5-HT ReceptorERKEpigenetic Reader DomainNicotinic acetylcholine receptorsSerotonin Receptor5-hydroxytryptamine ReceptorExtracellular signal regulated kinasesacetylcholinehuman α7 nAChRalzheimer diseaseGSK-3βCREBERK1/2rat α7 nAChRschizophrenia5-HT3 receptorα7 neuronal nicotinic acetylcholine receptorInhibitorinhibitorinhibit

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