CX 546
(Synonyms: 苯并二氧六环-6-(1-哌啶基)甲酰胺) 目录号 : GC14495
CX 546是一种强效的3-羟基-5-甲基-4-异唑丙酸（AMPA）受体激活剂，EC50值为93.2µM。
Cas No.:215923-54-9
Sample solution is provided at 25 µL, 10mM.
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CX 546 is a potent activator of 3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, with an EC50 value of 93.2µM[1]. CX 546 greatly prolonged the duration of synaptic responses and hippocampal excitatory postsynaptic currents in animals[2]. CX 546 has been widely used as a regulator of central nervous system functions and is involved in influencing various energy metabolism pathways[3].
In vitro, CX 546 treatment at 50μM for 48 hours led to an increase in cell proliferation and enhanced viability in subventricular zone (SVZ) cells of mice[4]. CX 546 treatment at 200μM for 72 hours reversed the inhibition of viability caused by cisplatin (10μM) and reduced cell death[5].
In,vivo, CX 546 treatment (0.5mg/kg/day) via intraperitoneally administration into the infarction rat model for 4 weeks exacerbated the infarction symptoms and tissue damage, activated the TLR4/NF-κB pathway, and impaired the cardiac function[6]. A single intraperitoneal injection of CX 546 at a dose of 16mg/kg into newborn rats can effectively reverse the respiratory depression caused by opioid drugs and barbiturate drugs within 60min[7]. Intraperitoneally injecting a single dose of CX 546 (10mg/kg) into the rat model could suppress chronic neuropathic pain caused by acute noxious stimulus within 5 minutes[8].
References:
[1] Pellerin L, Magistretti P J. Ampakine™ CX546 bolsters energetic response of astrocytes: a novel target for cognitive‐enhancing drugs acting as α‐amino‐3‐hydroxy‐5‐methyl‐4‐isoxazolepropionic acid (AMPA) receptor modulators[J]. Journal of neurochemistry, 2005, 92(3): 668-677.
[2] Arai A C, Xia Y F, Rogers G, et al. Benzamide-type AMPA receptor modulators form two subfamilies with distinct modes of action[J]. The Journal of pharmacology and experimental therapeutics, 2002, 303(3): 1075-1085.
[3] Nagarajan N, Quast C, Boxall A R, et al. Mechanism and impact of allosteric AMPA receptor modulation by the AmpakineTM CX546[J]. Neuropharmacology, 2001, 41(6): 650-663.
[4] Schitine C, Xapelli S, Agasse F, et al. Ampakine CX546 increases proliferation and neuronal differentiation in subventricular zone stem/progenitor cell cultures[J]. European Journal of Neuroscience, 2012, 35(11): 1672-1683.
[5] Lomeli N, Pearre D C, Cruz M, et al. Cisplatin induces BDNF downregulation in middle-aged female rat model while BDNF enhancement attenuates cisplatin neurotoxicity[J]. Experimental neurology, 2024, 375: 114717.
[6] Li Z, Yu Z, Cui S, et al. AMPA receptor inhibition alleviates inflammatory response and myocardial apoptosis after myocardial infarction by inhibiting TLR4/NF-κB signaling pathway[J]. International Immunopharmacology, 2024, 133: 112080.
[7] Ren J, Poon B Y, Tang Y, et al. Ampakines alleviate respiratory depression in rats[J]. American journal of respiratory and critical care medicine, 2006, 174(12): 1384-1391.
[8] Talay R S, Liu Y, Michael M, et al. Pharmacological restoration of anti-nociceptive functions in the prefrontal cortex relieves chronic pain[J]. Progress in neurobiology, 2021, 201: 102001.
CX 546是一种强效的3-羟基-5-甲基-4-异唑丙酸（AMPA）受体激活剂，EC50值为93.2µM[1]。CX 546能显著延长动物突触响应时间及海马兴奋性突触后电流[2]。CX 546被广泛应用于中枢神经系统功能调节，并参与多种能量代谢通路的调控[3]。
在体外，50μM浓度的CX 546处理48小时可促进小鼠脑室下区（SVZ）细胞增殖并增强细胞活力[4]。200μM的CX 546处理72小时能逆转顺铂（10μM）引起的细胞活力抑制并减少细胞死亡[5]。
在体内，梗死大鼠模型经腹腔注射CX 546（0.5mg/kg/day）4周后，梗死症状和组织损伤加剧，TLR4/NF-κB通路被激活，心脏功能受损[6]。给新生大鼠腹腔注射16mg/kg 单剂量的CX 546可在60分钟内有效逆转阿片类药物和巴比妥类药物引起的呼吸抑制[7]。给大鼠模型单次腹腔注射10mg/kg剂量的CX 546能在5分钟内抑制急性伤害性刺激引发的慢性神经病理性疼痛[8]。
| Cell experiment [1]: | |
Cell lines | OVCAR8 cells |
Preparation Method | The established OVCAR8 cell line was cultured in RPMI 1640 medium, which contained 300mg/L l-glutamine, 10% fetal bovine serum and 1× penicillin/streptomycin. The cells were seeded at a density of approximately 1 × 104 cells per well in transparent 96-well plates, with a final volume of 200μL. The culture plates were incubated at 37 °C and 5% CO2 exposed to 10μM Cisplatin with or without increasing concentrations of CX 546 (50μM, 100μM, 200μM, 300μM) for 72 hours. Cell viability was determined using a cell viability kit. |
Reaction Conditions | 50μM, 100μM, 200μM, 300μM; 72h |
Applications | CX 546 significantly reversed the inhibition of viability caused by cisplatin in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley (SD) rats |
Preparation Method | Male Sprague-Dawley (SD) rats were raised in a pathogen-free environment with a temperature of 20-22 °C and a relative humidity of 50-55%. The rats had free access to food and water. The rats were randomly divided into the following four groups: (1) Sham group; (2) Myocardial infarction group (MI), with the left coronary artery (left anterior descending branch [LAD]) ligated; (3) MI + CX 546 treatment group (MI + CX); (4) MI + NBQX treatment group (MI + NB). The second, third, and fourth groups underwent LAD ligation surgery. The rats that underwent the surgery were anesthetized intraperitoneally with a 3% pentobarbital sodium solution (2mL/kg) and had their tracheas intubated to support breathing. The Sham group only sutured the heart without ligation. The remaining rats underwent open-chest surgery and then ligated the left anterior descending branch (LAD), followed by closing the chest. The successful induction of the myocardial infarction model was confirmed by observing ST segment elevation on the electrocardiogram recorder or the appearance of pale areas in the proximal ventricular region at the distal end of the ligated line. After the surgery, all rats were intramuscularly injected with penicillin (200,000IU/day) for one week. CX 546 (0.5mg/kg/day) and NBQX (1mg/kg/day) were intraperitoneally injected into rats in groups (3) and (4) for 4 consecutive weeks after performing the LAD ligation procedure. The rats were anesthetized with a lethal dose and sacrificed, and their hearts were removed and rapidly fixed in 4% paraformaldehyde solution for more than 24 hours. The fixed heart tissues were embedded in paraffin and cut into 5μm thick sections. Masson's trichrome staining was used to observe the morphology of the heart tissue and evaluate the degree of fibrosis in the infarcted myocardium. |
Dosage form | 0.5mg/kg/day for 4 weeks; i.p. |
Applications | CX 546 treatment exacerbated the symptoms and tissue damage of the infarction in infarcted rats. |
References: | |
| Cas No. | 215923-54-9 | SDF | |
| 别名 | 苯并二氧六环-6-(1-哌啶基)甲酰胺 | ||
| 化学名 | (2,3-dihydrobenzo[b][1,4]dioxin-6-yl)(piperidin-1-yl)methanone | ||
| Canonical SMILES | O=C(C1=CC=C2OCCOC2=C1)N3CCCCC3 | ||
| 分子式 | C14H17NO3 | 分子量 | 247.29 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0438 mL | 20.2192 mL | 40.4384 mL |
| 5 mM | 0.8088 mL | 4.0438 mL | 8.0877 mL |
| 10 mM | 0.4044 mL | 2.0219 mL | 4.0438 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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