SCH 58261
目录号 : GC14565
SCH 58261是一种强效选择性非黄嘌呤类A2A腺苷受体拮抗剂，IC50值为15nM。
Cas No.:160098-96-4
Sample solution is provided at 25 µL, 10mM.
SCH 58261 is a potent and selective non-xanthine A2A adenosine antagonist, with an IC50 of 15nM[1]. SCH 58261 has been widely used in animal models of cardiovascular and neurological regulation[2].
In vitro, SCH 58261 treatment (50nM; 24h) reduced microglia proliferation as well as the expression and release of pro-inflammatory mediators in rat retinal nerve cell culture[3].
In vivo, SCH 58261 treatment at a single dose of 5mg/kg (i.p.) for 90min reversed reserpine-induced muscle stiffness and attenuated reserpine-enhanced tonic and reflex electromyographic activity in gastrocnemius and tibial muscles[4]. Systemic administration of SCH 58261 (5mg/kg; i.p.; 3 times, every 3h, 10min before haloperidol) within one day partially decreased the haloperidol-induced catalepsy and the increase in the proenkephalin (PENK) expression in both dorsolateral and ventrolateral parts of the striatum of rats[5]. In rats, intraperitoneal injection of SCH 58261 at a single dose of 10mg/kg for one day enhanced exercise capacity, increased alertness, and slightly increased blood pressure and heart rate[6]. Intraperitoneal injection of SCH 58261 (0.01mg/kg) administered 5 minutes after middle cerebral artery occlusion (MCAO) inhibited turning behavior in rats and significantly reduced the outflow of glutamate, markedly decreasing cortical damage without preventing sensorimotor impairment[7].
References:
[1] Zocchi C, Ongini E, Conti A, et al. The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist[J]. The Journal of pharmacology and experimental therapeutics, 1996, 276(2): 398-404.
[2] Monopoli A, Casati C, Lozza G, et al. Cardiovascular pharmacology of the A2A adenosine receptor antagonist, SCH 58261, in the rat[J]. The Journal of pharmacology and experimental therapeutics, 1998, 285(1): 9-15.
[3] Aires I D, Boia R, Rodrigues‐Neves A C, et al. Blockade of microglial adenosine A2A receptor suppresses elevated pressure‐induced inflammation, oxidative stress, and cell death in retinal cells[J]. Glia, 2019, 67(5): 896-914.
[4] Wardas J, Konieczny J, Lorenc‐Koci E. SCH 58261, an A2A adenosine receptor antagonist, counteracts parkinsonian‐like muscle rigidity in rats[J]. Synapse, 2001, 41(2): 160-171.
[5] Wardas J, Pietraszek M, Dziedzicka-Wasylewska M. SCH 58261, a selective adenosine A2A receptor antagonist, decreases the haloperidol-enhanced proenkephalin mRNA expression in the rat striatum[J]. Brain research, 2003, 977(2): 270-277.
[6] Ongini E. SCH 58261: A selective A2A adenosine receptor antagonists[J]. Drug development research, 1997, 42(2): 63-70.
[7] Melani A, Pantoni L, Bordoni F, et al. The selective A2A receptor antagonist SCH 58261 reduces striatal transmitter outflow, turning behavior and ischemic brain damage induced by permanent focal ischemia in the rat[J]. Brain Research, 2003, 959(2): 243-250.
SCH 58261是一种强效选择性非黄嘌呤类A2A腺苷受体拮抗剂，IC50值为15nM[1]。SCH 58261已广泛应用于心血管和神经调节的动物模型研究[2]。
在体外，50nM浓度的SCH 58261处理24小时可抑制大鼠视网膜神经细胞培养物中小胶质细胞的增殖，并减少促炎介质的表达和释放[3]。
在体内，单次腹腔注射5mg/kg剂量的SCH 58261 90分钟后，能逆转利血平诱导的肌肉僵硬，并减轻利血平增强的腓肠肌和胫骨肌强直及反射性肌电活动[4]。一日内以5mg/kg剂量腹腔注射三次SCH 58261（每次间隔3小时，于氟哌啶醇给药前10分钟注射），可部分缓解氟哌啶醇诱导的大鼠纹状体背外侧和腹外侧区的强直症及前脑啡肽原（PENK）表达升高[5]。单次腹腔注射10mg/kg剂量的SCH 58261一天后，可增强大鼠的运动能力、提高警觉性，并轻微升高血压和心率[6]。在大脑中动脉闭塞（MCAO）后5分钟腹腔注射0.01mg/kg剂量的SCH 58261，能抑制大鼠翻身行为，显著减少谷氨酸流出，明显减轻皮质损伤，无法改善感觉运动功能障碍[7]。
| Cell experiment [1]: | |
Cell lines | Rat primary retinal neural cell |
Preparation Method | Primary retinal neural cell cultures were prepared from 3 to 5-day-old Wistar rats. The cells were plated at a density of 2×106 cells/cm2 in 12‐well plates with glass coverslips, all precoated with poly‐d‐lysine (0.1mg/mL). Cells were cultured at 37°C in a humidified atmosphere of 5% CO2 for 7 days. Cell cultures were incubated with 50nM of the SCH 58261 for 45min before placing the cultures inside the pressure chamber. Cultures were submitted to elevated hydrostatic pressure (EHP; 70 mmHg above atmospheric pressure) for 24h. The morphology and proliferation ability of the cells were analyzed. |
Reaction Conditions | 50nM; 24h |
Applications | SCH 58261 treatment prevented cell morphological changes and reduced cell death caused by high pressure in rat primary retinal neural cells. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | Male Wistar rats weighing 270-290g were used and kept 3 rats per cage with free access to food and water. All rats were kept on a 12-h light/dark cycle (lights on at 8: 00 am) in standardized temperature, humidity and light conditions with free access to food and water. Focal cerebral ischemia was produced by a permanent middle cerebral artery occlusion (MCAO) in the right hemisphere. Rats were anesthetized with 5.0% isoflurane and spontaneously inhaled 1.0 to 2.0% isoflurane in air by use of a mask. Body core temperature was maintained at 37 °C with the recirculating pad and K module and monitored via an intrarectal type T thermocouple. The rats were placed in a stereotaxic frame and the surgical procedure to occlude MCAO consisted of the insertion of a 4-0 nylon monofilament, pre-coated with silicone mixed with a hardener, via the external carotid artery into the internal carotid artery to block the origin of MCAO. Sham-operated rats were used as control in which the filament was inserted into the internal carotid artery and then withdrawn. After the end of the surgical procedure anesthesia was discontinued, the rats were placed in a prone position, and were then allowed to recover from anesthesia. Recovery from anesthesia lasted for about 15min, thereafter, rats had free access to food and water. SCH 58261 was dissolved by sonication in saline with 1% Tween 80. In SCH 58261-treated and vehicle-treated rats, the SCH 58261 or vehicle was administered intraperitoneally 5min at a dose of 0.01mg/kg once after occlusion. Rats were sacrificed after one day from the experiment and brain tissues were collected for histological analysis. |
Dosage form | 0.01mg/kg for once; i.p. |
Applications | SCH 58261 treatment significantly improved the neurological deficit and reduced ischemic damage in the striatum and cortex of rats. |
References: | |
| Cas No. | 160098-96-4 | SDF | |
| 化学名 | 2-(furan-2-yl)-7-phenethyl-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine | ||
| Canonical SMILES | NC1=NC(N(CCC2=CC=CC=C2)N=C3)=C3C4=NC(C5=CC=CO5)=NN41 | ||
| 分子式 | C18H15N7O | 分子量 | 345.36 |
| 溶解度 | ≥ 34.5mg/mL in DMSO | 储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8955 mL | 14.4776 mL | 28.9553 mL |
| 5 mM | 579.1 μL | 2.8955 mL | 5.7911 mL |
| 10 mM | 289.6 μL | 1.4478 mL | 2.8955 mL |
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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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工作液浓度： mg/ml；
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2.
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