Bifeprunox (mesylate)
(Synonyms: 7-[4-([1,1'-联苯]-3-甲基)-1-哌嗪基]-2(3H)H-苯并恶唑酮甲磺酸) 目录号 : GC46014
An atypical antipsychotic
Cas No.:350992-13-1
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
Bifeprunox is an atypical antipsychotic.1 It is a dopamine D2 receptor partial agonist and an agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Kis = 2.2 and 9.3 nM, respectively).2,3 Bifeprunox inhibits apomorphine-induced climbing behavior in mice (ED50 = 0.1 mg/kg) and the conditioned avoidance response in rats (ED50 = 0.8 mg/kg).3 It decreases basal prepulse inhibition of the acoustic startle response in rats by 42% when administered at a dose of 10 mg/kg.2
|1. Wadenberg, M.-L.G. Bifeprunox: A novel antipsychotic agent with partial agonist properties at dopamine D2 and serotonin 5-HT1A receptors. Future Neurol. 2(2), 153-165 (2007).|2. Auclair, A.L., Galinier, A., Besnard, J., et al. Putative antipsychotics with pronounced agonism at serotonin 5-HT1A and partial agonist activity at dopamine D2 receptors disrupt basal PPI of the startle reflex in rats. Psychopharmacol. (Berl). 193(1), 45-54 (2007).|3. Feenstra, R.W., de Moes, J., Hofma, J.J., et al. New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D2-receptor and serotonin 5-HT1A-receptor affinities. Bioorg. Med. Chem. Lett. 11(17), 2345-2349 (2001).
| Cas No. | 350992-13-1 | SDF | |
| 别名 | 7-[4-([1,1'-联苯]-3-甲基)-1-哌嗪基]-2(3H)H-苯并恶唑酮甲磺酸 | ||
| Canonical SMILES | O=C1NC2=CC=CC(N3CCN(CC4=CC(C5=CC=CC=C5)=CC=C4)CC3)=C2O1.CS(=O)(O)=O | ||
| 分子式 | C24H23N3O2.CH3SO3H | 分子量 | 481.6 |
| 溶解度 | DMSO : 8.6 mg/mL (17.86 mM; Need ultrasonic and warming) | 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 | 2.0764 mL | 10.3821 mL | 20.7641 mL |
| 5 mM | 0.4153 mL | 2.0764 mL | 4.1528 mL |
| 10 mM | 0.2076 mL | 1.0382 mL | 2.0764 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Bifeprunox: a partial agonist at dopamine D2 and serotonin 1A receptors, influences nicotine-seeking behaviour in response to drug-associated stimuli in rats
Addict Biol 2012 Mar;17(2):274-86.PMID:21521422DOI:10.1111/j.1369-1600.2011.00319.x.
Environmental stimuli repeatedly associated with the self-administered drugs may acquire motivational importance. Because dopamine (DA) D(2) /D(3) partial agonists and D(3) antagonists interfere with the ability of drug-associated cues to induce drug-seeking behaviour, the present study investigated whether Bifeprunox, 7-[4-([1,1'biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone mesylate), a high-affinity partial agonist of the D(2) subfamily of DA receptors and of serotonin(1A) receptors, influences reinstatement of drug-associated cue-induced nicotine-seeking behaviour. The study also explored whether Bifeprunox reduced motivated behaviour by evaluating its effects on reinstatement induced by stimuli conditioned to sucrose. To verify whether Bifeprunox interferes with the primary reinforcing properties of either drug or sucrose, we compared its effects on nicotine self-administration and on sucrose-reinforced behaviour. Different groups of experimentally naïve, food-restricted Wistar rats were trained to associate a discriminative stimulus with response-contingent availability of nicotine or sucrose and tested for reinstatement after extinction of nicotine or sucrose-reinforced behaviour. Bifeprunox (4-16 µg/kg, s.c.) dose-dependently attenuated the response-reinstating effects of nicotine-associated cues. Higher doses (64-250 µg/kg, s.c.) reduced spontaneous locomotor activity and suppressed operant responding induced by sucrose-associated cues and by the primary reinforcing properties of nicotine or sucrose. Provided they can be extrapolated to abstinent human addicts, these results suggest the potential therapeutic use of partial DA D(2) receptor agonist to prevent cue-controlled nicotine-seeking and relapse. The profile of action of high doses of Bifeprunox remains to be examined for potential sedation or anhedonia effects.