Pentiapine (CGS 10746)
(Synonyms: 喷硫平,CGS 10746) 目录号 : GC33730
Pentiapine (CGS 10746) (CGS 10746) 是一种多巴胺释放抑制剂，不与突触多巴胺受体位点结合。
Cas No.:81382-51-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Two hundred and fifty-seven male mice are used in this study. Animals are divided into 19 groups (n=8). The first group receives physiological saline, the second receives 40 mg/kg of morphine and the other eight groups receive 0.5, 1, 2, 4, 8, 16, 24 or 32 mg/kg of Pentiapine, respectively. The remaining groups receive an injection of morphine and 30 min afterwards, an injection of physiological saline, 0.5, 1, 2, 4, 8, 16, 24 or 32 mg/kg of Pentiapine, respectively. In the groups receiving only one injection, animals are placed onto the sensory plates for a period of 90 min immediately after treatment. The computer registers the activity each 15 min. In the groups receiving two injections, animals are placed onto the sensory plates immediately after the first injection for a period of 30 min then after the second injection the motor activity is registered at 15, 30, 45 and 60 min[1]. |
References: [1]. Manzanedo C, et al. Effects of CGS 10746B on hyperactivity and place preference induced by morphine. Behav Brain Res. 2001 Nov 29;126(1-2):23-32. | |
Pentiapine is a novel dopamine release inhibitor.
Pentiapine is a novel dopamine release inhibitor.The results show that Pentiapine dose-dependently reduces motor activity of mice. Moreover, Pentiapine dose-dependently reduces morphine-induced hyperactivity. Newman-Keuls post-hoc comparisons indicate that the group receiving morphine plus saline presents more activity than the groups receiving morphine plus 2 (P<0.05), 4, 8, 16, 24 and 32 (P<0.01) mg/kg of Pentiapine. Moreover, the groups receiving morphine plus 0.5, 1 and 2 mg/kg of Pentiapine present more activity than the groups receiving morphine plus 4, 8, 16, 24 and 32 mg/kg of Pentiapine (P<0.01)[1]. 30 mg/kg dose of Pentiapine completely blocks the methylenedioxymethamphetamine (MDMA) conditioned place preference (CPP) and also blocks the establishment of a cocaine CPP[2].
[1]. Manzanedo C, et al. Effects of CGS 10746B on hyperactivity and place preference induced by morphine. Behav Brain Res. 2001 Nov 29;126(1-2):23-32. [2]. Bilsky EJ, et al. CGS 10746B, a novel dopamine release inhibitor, blocks the establishment of cocaine and MDMA conditioned place preferences. Pharmacol Biochem Behav. 1998 Jan;59(1):215-20.
| Cas No. | 81382-51-6 | SDF | |
| 别名 | 喷硫平,CGS 10746 | ||
| Canonical SMILES | CN1CCN(C2=NC3=CC=CC=C3SC4=NC=CN42)CC1 | ||
| 分子式 | C15H17N5S | 分子量 | 299.39 |
| 溶解度 | DMSO: 100 mg/mL (334.01 mM) | 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 | 3.3401 mL | 16.7006 mL | 33.4012 mL |
| 5 mM | 0.668 mL | 3.3401 mL | 6.6802 mL |
| 10 mM | 0.334 mL | 1.6701 mL | 3.3401 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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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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Presynaptic inhibition of nigrostriatal dopamine release in the mouse: lack of cross tolerance between apomorphine, GBL and CGS 10746B
Life Sci 1988;42(16):1503-6.PMID:3352463DOI:10.1016/0024-3205(88)90006-9
Acute parenteral injections of apomorphine, gamma-butyrolactone (GBL) and CGS 10746B decreased dopamine release in the mouse nigrostriatal pathway as evidenced by decreases in striatal 3-methoxytyramine levels. In a 7 day treatment paradigm, the effects of acute apomorphine, GBL and CGS 10746B were unaltered in animals treated b.i.d. with GBL (500 mg/kg, i.p.). In contrast, the actions of acute CGS 10746B expressed a complete tolerance in mice treated b.i.d. with CGS 10746B (20 mg/kg, i.p.), while the actions of acute apomorphine or GBL were similar in the chronic saline and chronic CGS 10746 groups. These data show that the inhibition of striatal dopamine release by CGS 10746B is susceptible to tolerance. In addition, the lack of cross tolerance between GBL, apomorphine and CGS 10746B suggests independent sites of action for these agents in inhibiting dopamine release.