S-8510 phosphate (SB-737552 phosphate)
(Synonyms: SB-737552 phosphate) 目录号 : GC31121
S-8510 (phosphate) 是一种反向苯二氮卓 (BDZ) 受体激动剂，对 -GABA 和 +GABA 的 Kis 分别为 34.6 nM、36.2 nM。
Cas No.:151466-23-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Mice, Rats[1]Proconvulsant actions of S-8510 are examined in combiition with a subconvulsive dose of convulsant (PTZ or strychnine) or minimal electroconvulsive shock in ddY mice. Each convulsant is administrated, simultaneously with the inverse agonist, whereas minimal electroconvulsive shock is applied 5 min after intravenous injection of the inverse agonist. The proconvulsant test of S-8510 on PTZ (52, 62.5, 75 or 90 mg/kg s.c.) or strychnine (0.25 mg/kg, s.c.)-induced convulsion is made. ED50 values for producing clonic convulsion to death in 50% of ddY mice are calculated. Anxiogenic actions of each inverse agonist are examined in the punished water licking method in Wistar rats. Each inverse agonist is administered per OS 30 min before the test trial. Antiamnesic actions of inverse agonists are examined in the water maze paradigm. Wistar rats are given 4 trials every day for consecutive 4 days. On the 5 th day, each animal has the retention test for 60 s. Amnesia is produced by intraperitoneally injected scopolamine at a dose of 0.5 mg/kg. Scopolamine and each inverse agonist are given 15 min and 30 min before the retention trial, respectively[1]. |
References: [1]. Kawasaki K, et al. A novel benzodiazepine inverse agonist, S-8510, as a cognitive enhancer. Prog Neuropsychopharmacol Biol Psychiatry. 1996 Nov;20(8):1413-25. | |
S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for -GABA and +GABA respectively.
S-8510 has a relatively high affinity to BDZ receptors. The ratio of Ki values for each ligand with and without GABA is defined as the GABA ratio, which is considered as a biochemical index for BDZ receptor ligands. The GABA ratio for S-8510 or CGS8216 is close to the value for flumazenil which is considered as an antagonist or a very weak agonist. S-8510 (10-7 M) enhances LTP and this enhancement is antagonized by BDZ receptor antagonist, flumazenil. Flumazenil itself does not atfect LTP or evokes responses prior to tetanic stimulation. S-8510 has no effect on the field evoked potential up to 10-5 M. However, S-8510 increases the amplitude of the population spike at a dose of 10-4 M, and this effect is completely antagonized by concomitant application of flumazenil (10-4 M) [1].
S-8510 or CGS8216 could cause lethal convulsion only in combination with more than 90 mg/kg of PTZ. The proconvulsant activity of S-8510 appears to be selective for PTZ-induced subconvulsive state. Scopolamine decreases the time spending in the area around the platform, indicating the amnesic action of scopolamine. S-8510 and CGS8216 reverses this scopolamine-induced amnesia. S-8510 improves the memory impairment induced by diazepam in the water maze and passive avoidance paradigms as well. S-8510 dose-dependently increases the ACh level up to 100 mg/kg. Both S-8510 and PTZ increases the extracellular level of NA in the hippocampus in a dose-dependent manner. Anxiogenic actions of S-8510, CGS8216 and FG7142 are examined in the water lick conflict paradigm of Wistar rats. S-8510 and CGS8216 fail to affect this behavioral paradigm up to 30 mg/kg. S-8510 significantly decreases the immobility time in the forced swimming test using ddY mice at 40 to 80 mg/kg in a dose-dependent manner. In the tetrabenazine-induced ptosis model, S-8510 significantly reduces the extent of ptosis induced by tetrabenazine at doses more than 10 mg/kg. Again, S-8510 reduces the extent of ptosis only by 39% even at the maximum dose, whereas imipramine exerts more pronounced effects (by about 80% at a dose of 20 mg/kg)[1].
[1]. Kawasaki K, et al. A novel benzodiazepine inverse agonist, S-8510, as a cognitive enhancer. Prog Neuropsychopharmacol Biol Psychiatry. 1996 Nov;20(8):1413-25.
| Cas No. | 151466-23-8 | SDF | |
| 别名 | SB-737552 phosphate | ||
| Canonical SMILES | O=P(O)(O)O.C12=NC=C3C(NC(C4=NOC=C4)=N3)=C1COCC2 | ||
| 分子式 | C12H13N4O6P | 分子量 | 340.23 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| 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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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9392 mL | 14.6959 mL | 29.3919 mL |
| 5 mM | 0.5878 mL | 2.9392 mL | 5.8784 mL |
| 10 mM | 0.2939 mL | 1.4696 mL | 2.9392 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
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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