Home>>Signaling Pathways>> Neuroscience>> Behavioral Neuroscience>>Bifeprunox (mesylate)

Bifeprunox (mesylate) Sale

(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

Bifeprunox (mesylate) Chemical Structure

Cas No.:350992-13-1

规格 价格 库存 购买数量
1mg
¥462.00
现货
5mg
¥1,268.00
现货
10mg
¥2,091.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

产品描述

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).

Chemical Properties

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 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。
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。

溶解性数据

制备储备液
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
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

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
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

Research Update

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.