2-Chloro-N6-cyclopentyladenosine
(Synonyms: 2-氯-N6-环戊基腺苷) 目录号 : GC11665An adenosine A1 receptor antagonist
Cas No.:37739-05-2
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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2-Chloro-N6-cyclopentyladenosine is a potent and selective agonist of adenosine A1 receptor [1].
The adenosine A1 receptor is a G protein-coupled receptor for adenosine and plays an important role in sleep promotion.
2-Chloro-N6-cyclopentyladenosine (CCPA) is a potent and selective agonist of adenosine A1 receptor. CCPA inhibited [3H]PIA binding to A1 receptors of rat brain membranes and [3H]NECA binding to A2 receptors of rat striatal membranes with Ki values of 0.4 and 3900 nM, respectively.
Also, CCPA inhibited adenylate cyclase in rat fat cell membranes with IC50 value of 33 nM and stimulated adenylate cyclase activity in human platelet membranes with EC50 value of 3500 nM [1]. In rat and bovine brain, CCPA exhibited high affinity for A1 receptors with Ki values of 1.3 and 0.5 nM, respectively. In spontaneously beating rat atria, CCPA inhibited chronotropic activity with EC50 value of 8.2 nM [2].
In ischemia/reperfusion rat model, CCPA significantly inhibited the rise of coronary perfusion pressure and diastolic pressure [2]. In rabbits, CCPA reduced mean blood pressure by 40-50% and also lowered heart rate [3]. In mice, CCPA (1.4-27.6 µmol/kg) increased [35S]TBPS binding in membranes from the substantia nigra, hippocampus, cerebral cortex and striatum mediated by A1 receptor. CCPA reduced GABA-coupled chloride channel function and induced anticonvulsant activity [4].
References:
[1]. Lohse MJ, Klotz KN, Schwabe U, et al. 2-Chloro-N6-cyclopentyladenosine: a highly selective agonist at A1 adenosine receptors. Naunyn Schmiedebergs Arch Pharmacol, 1988, 337(6): 687-689.
[2]. Monopoli A, Conti A, Dionisotti S, et al. Pharmacology of the highly selective A1 adenosine receptor agonist 2-chloro-N6-cyclopentyladenosine. Arzneimittelforschung, 1994, 44(12): 1305-1312.
[3]. Concas A, Santoro G, Mascia MP, et al. Anticonvulsant doses of 2-chloro-N6-cyclopentyladenosine, an adenosine A1 receptor agonist, reduce GABAergic transmission in different areas of the mouse brain. J Pharmacol Exp Ther, 1993, 267(2): 844-851.
[4]. Sandoli D, Chiu PJ, Chintala M, et al. In vivo and ex vivo effects of adenosine A1 and A2 receptor agonists on platelet aggregation in the rabbit. Eur J Pharmacol, 1994, 259(1): 43-49.
Cas No. | 37739-05-2 | SDF | |
别名 | 2-氯-N6-环戊基腺苷 | ||
化学名 | (2R,3R,4S,5R)-2-(2-chloro-6-(cyclopentylamino)-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol | ||
Canonical SMILES | ClC(N=C12)=NC(NC3CCCC3)=C2N=CN1[C@@H]([C@@H]4O)O[C@H](CO)[C@H]4O | ||
分子式 | C15H20ClN5O4 | 分子量 | 369.81 |
溶解度 | <36.98mg/ml in ethanol; <36.98mg/ml in DMSO | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.7041 mL | 13.5205 mL | 27.0409 mL |
5 mM | 0.5408 mL | 2.7041 mL | 5.4082 mL |
10 mM | 0.2704 mL | 1.352 mL | 2.7041 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
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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工作液浓度: mg/ml;
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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