Sumanirole maleate
(Synonyms: U-95666E; PNU-95666) 目录号 : GC37702
A dopamine D2 receptor agonist
Cas No.:179386-44-8
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
Sumanirole is a dopamine D2 receptor agonist that is selective for D2 over D1, D3, and D4 receptors (Kis = 9.0, >7,140, 1,940, and >2,190 nM, respectively).1 It inhibits forskolin-stimulated cAMP accumulation in CHO cells expressing human recombinant D2A receptors (EC50 = 17 nM). Sumanirole decreases plasma prolactin levels in rats when administered at doses greater than or equal to 3.1 ?mol/kg and inhibits dopamine neuron firing in the substantia nigra pars compacta (SNPC) in anesthetized rats (ED50 = 2.3 ?mol/kg). Sumanirole (≥12.5 ?mol/kg, s.c.) increases horizontal locomotor activity in a reserpinized, α-methyl-para-tyrosine (AMPT) rat model of Parkinson's disease. It also decreases time spent in the open arms of the elevated plus maze and time spent immobile in the forced swim test, indicating anxiolytic- and antidepressant-like activities, respectively, in mice with SNPC lesions when administered at a dose of 0.1 mg/kg.2 Sumanirole (≥0.1 mg/kg, s.c.) reduces premature responding, a measure of impulsivity, by rats in the 5-choice serial reaction time test (5CRTT) compared with untreated animals.3
1.McCall, R.B., Lookingland, K.J., Bédard, P.J., et al.Sumanirole, a highly dopamine D2-selective receptor agonist: In vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's diseaseJ. Pharmacol. Exp. Ther.314(3)1248-1256(2005) 2.Carcinella, S., Drui, G., Boulet, S., et al.Implication of dopamine D3 receptor activation in the reversion of Parkinson's disease-related motivational deficitsTransl. Psychiatry4(6)e401(2014) 3.Fernando, A.B., Economidou, D., Theobald, D.E., et al.Modulation of high impulsivity and attentional performance in rats by selective direct and indirect dopaminergic and noradrenergic receptor agonistsPsychopharmacology (Berl.)219(2)341-352(2012)
| Cas No. | 179386-44-8 | SDF | |
| 别名 | U-95666E; PNU-95666 | ||
| Canonical SMILES | O=C1NC2=C3N1C[C@H](NC)CC3=CC=C2.O=C(/C=C\C(O)=O)O | ||
| 分子式 | C15H17N3O5 | 分子量 | 319.31 |
| 溶解度 | DMSO: 50 mg/mL (156.59 mM); Water: 10 mg/mL (31.32 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 | 3.1318 mL | 15.6588 mL | 31.3175 mL |
| 5 mM | 0.6264 mL | 3.1318 mL | 6.2635 mL |
| 10 mM | 0.3132 mL | 1.5659 mL | 3.1318 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。
Differential effects of D1 and D2 dopamine agonists on memory, motivation, learning and response time in non-human primates
Eur J Neurosci 2019 Jan;49(2):199-214.PMID:30326151DOI:10.1111/ejn.14208.
Dopamine (DA) plays a critical role in cognition, motivation and information processing. DA action has been shown to both improve and/or impair cognition across different receptor types, species, subjects and tasks. This complex relationship has been described as an inverted U-shaped function and may be due to the differential effects of DA receptor activation in the striatum and prefrontal cortex. We have investigated the effects of selective DA agonists on cognitive performance in healthy monkeys using a touch screen running tasks from the CAmbridge Neuropsychological Test Automated Battery (CANTAB). One of two DA agonist drugs or placebo was administered prior to each daily CANTAB session: Dihydrexidine hydrochloride (selective D1 agonist, 0.4-0.9 mg/kg), or Sumanirole maleate (selective D2 agonist 0.05-0.3 mg/kg). Three CANTAB tasks were tested: (a) "self-ordered sequential search task" which tested spatial working memory, (b) "reversal learning task," which tested association learning, cognitive flexibility and attention and (c) "visually guided reaching task," which tested reaction time and accuracy. At high dosages, the D2 agonist improved spatial working memory performance, while impairing reversal learning and slowing reach response latency. No consistent cognitive effects were observed with the D1 agonist across the dosages tested. A significant decrease in trial completion rate was observed at the higher dosages of both the D1 and D2 agonists which were consistent with decreased motivation. These results are consistent with task-specific effects of a D2 agonist as well as dose specific insensitivities of a D1 agonist on cognitive and motor behaviors in a healthy monkey.
Effect of GDNF on depressive-like behavior, spatial learning and key genes of the brain dopamine system in genetically predisposed to behavioral disorders mouse strains
Behav Brain Res 2014 Nov 1;274:1-9.PMID:25101543DOI:10.1016/j.bbr.2014.07.045.
The effect of glial cell line-derived neurotrophic factor (GDNF) on behavior and brain dopamine system in predisposed to depressive-like behavior ASC (Antidepressant Sensitive Cataleptics) mice in comparison with the parental "nondepressive" CBA mice was studied. In 7days after administration (800ng, i.c.v.) GDNF decreased escape latency time and the path traveled to reach hidden platform in Morris water maze in ASC mice. GDNF enhanced depressive-like behavioral traits in both "nondepressive" CBA and "depressive" ASC mice. In CBA mice, GDNF decreased functional response to agonists of D1 (chloro-APB hydrobromide) and D2 (Sumanirole maleate) receptors in tail suspension test, reduced D2 receptor gene expression in the substantia nigra and increased monoamine oxydase A (MAO A) gene expression in the striatum. GDNF increased D1 and D2 receptor genes expression in the nucleus accumbens of ASC mice but failed to alter expression of catechol-O-methyltransferase, dopamine transporter, MAO B and tyrosine hydroxylase genes in both investigated mouse strains. Thus, GDNF produced long-term genotype-dependent effect on behavior and the brain dopamine system. GDNF pretreatment (1) reduced D1 and D2 receptors functional responses and D2 receptor gene expression in s. nigra of CBA mice; (2) increased D1 and D2 receptor genes expression in n. accumbens of ASC mice and (3) improved spatial learning in ASC mice. GDNF enhanced depressive-like behavior both in CBA and ASC mice. The data suggest that genetically defined variance in the cross-talk between GDNF and brain dopamine system contributes to the variability of GDNF-induced responses and might be responsible for controversial GDNF effects.