Picamilon
(Synonyms: 匹卡米隆,Nicotinoyl-GABA; Nicotinoyl-γ-aminobutyric acid) 目录号 : GC46206
A GABA derivative
Cas No.:34562-97-5
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
Picamilon is a derivative of γ-aminobutyric acid (GABA).1 It increases parietal cortical blood flow in rats and rabbits when administered at doses of 50 mg/kg, i.p. and 10 mg/kg, i.v., respectively.2 Picamilon (10 mg/kg) increases latency to enter the dark compartment in the passive avoidance conditioned reflex test in rats compared with control animals, indicating nootropic effects.1
|1. Kopelevich, V.M., Bulanova, L.N., Grigor'ev, I.A., et al. Synthesis and study of psychotropic and hypotensive properties of new picamilon derivatives. Pharm. Chem. J. 31(10), 536-539 (1997).|2. Mirzoyan, R.S., Gan'shina, T.S., Kosoi, M.Y., et al. Effect of picamilon on the cerebral cortical blood supply and microcirculation in the pial arteriolar system. Biull. Eksp. Biol. Med. 107(5), 668-670 (1989).
| Cas No. | 34562-97-5 | SDF | |
| 别名 | 匹卡米隆,Nicotinoyl-GABA; Nicotinoyl-γ-aminobutyric acid | ||
| Canonical SMILES | O=C(NCCCC(O)=O)C1=CN=CC=C1 | ||
| 分子式 | C10H12N2O3 | 分子量 | 208.2 |
| 溶解度 | DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:9): 0.10 mg/ml | 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 | 4.8031 mL | 24.0154 mL | 48.0307 mL |
| 5 mM | 0.9606 mL | 4.8031 mL | 9.6061 mL |
| 10 mM | 0.4803 mL | 2.4015 mL | 4.8031 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。
Picamilon, a γ-aminobutyric acid (GABA) analogue and marketed nootropic, is inactive against 50 biological targets
Basic Clin Pharmacol Toxicol 2023 Apr;132(4):355-358.PMID:36668678DOI:10.1111/bcpt.13836.
Picamilon is an analogue of the neurotransmitter γ-aminobutyric acid (GABA), which is marketed as a nootropic claiming to enhance cognition. There is a lack of in silico, in vitro and in vivo data on the safety of Picamilon. Therefore, to ascertain potential physiological effects of Picamilon, it was screened against 50 safety-related biological targets (receptors, ion channels, enzymes and transporters) by in silico and in vitro methods. Using two in silico tools, Picamilon was not predicted to bind to the targets. Similarly, Picamilon exhibited weak or no binding to the targets when measured in vitro at 10 μM. Overall, this data shows that Picamilon, although structurally similar to other GABA analogues, has a different biological target binding profile. Picamilon's lack of binding to the 50 targets fills important data gaps among GABA analogues, a group of structurally related substances found in drugs and other consumer products.
Identification and quantification of vinpocetine and Picamilon in dietary supplements sold in the United States
Drug Test Anal 2016 Mar-Apr;8(3-4):334-43.PMID:26426301DOI:10.1002/dta.1853.
Vinpocetine and Picamilon are drugs prescribed in many countries to treat a variety of cerebrovascular disorders. In the United States, vinpocetine and Picamilon have never been approved by the US Food and Drug Administration, but they are both available for sale directly to consumers as dietary supplements. We designed our study to determine the accuracy of supplement labels with regard to the presence and quantity of vinpocetine and Picamilon. A validated ultra-high performance liquid chromatography-photodiode-array method was developed for the quantification of vinpocetine and Picamilon. The separation was achieved using a reversed phase (C-18) column, photodiode array detection, and water/acetonitrile as the mobile phase. Vinpocetine and Picamilon were detected at concentrations as low as 10 and 50 ng/mL, respectively. The presence of vinpocetine and Picamilon was confirmed using reference standards. Twenty-three supplements labelled as containing vinpocetine were available for sale at two large supplement retail chains; 17 contained vinpocetine with quantities ranging from 0.3 to 32 mg per recommended daily serving. No vinpocetine was detected in six of the sampled supplements. The supplement label implied that vinpocetine was a constituent of lesser periwinkle in three of the supplements. Of the 31 Picamilon supplements available for sale from a variety of retailers: 30 contained Picamilon in quantities ranging from 2.7 to 721.5 mg per recommended daily serving. We found that consumers cannot obtain accurate information from supplement labels regarding the presence or quantity of vinpocetine and Picamilon. Copyright © 2015 John Wiley & Sons, Ltd.
Determination of Picamilon concentration in human plasma by liquid chromatography-tandem mass spectrometry
J Chromatogr B Analyt Technol Biomed Life Sci 2010 May 1;878(15-16):1181-4.PMID:20359966DOI:10.1016/j.jchromb.2010.03.013.
A rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the determination of Picamilon concentration in human plasma. Picamilon was extracted from human plasma by protein precipitation. High performance liquid chromatography separation was performed on a Venusil ASB C(18) column with a mobile phase consisting of methanol -10mM ammonium acetate-formic acid (55:45:01, v/v/v) at a flow rate of 0.65ml/min. Acquisition of mass spectrometric data was performed in selected reaction monitoring mode, using the transitions of m/z 209.0-->m/z (78.0+106.0) for Picamilon and m/z 152.0-->m/z (93.0+110.0) for paracetamol (internal standard). The method was linear in the concentration range of 1.00-5000ng/ml for the analyte. The lower limit of quantification was 1.00ng/ml. The intra- and inter-assay precision were below 13.5%, and the accuracy was between 99.6% and 101.6%. The method was successfully applied to characterize the pharmacokinetic profiles of Picamilon in healthy volunteers. This validated LC-MS/MS method was selective and rapid, and is suitable for the pharmacokinetic study of Picamilon in humans.
[Treatment of patients with chronic cerebral ischemia: experience of using the combined neuroprotective drug Picamilon Ginkgo]
Zh Nevrol Psikhiatr Im S S Korsakova 2022;122(9):95-103.PMID:36168693DOI:10.17116/jnevro202212209195.
Objective: To compare the clinical efficacy and safety of Picamilon Ginkgo and ginkgo biloba in patients with cognitive impairment in vascular diseases of the brain (chronic cerebral ischemia). Material and methods: An open multicenter randomized comparative study involved 278 patients over 45 years of age with a diagnosis of chronic cerebral ischemia and cognitive impairment. 139 of them received Picamilon Ginkgo and 139 received monotherapy with ginkgo biloba extract for 90 days. Dynamics were compared on the MoCA, MMSE, Hamilton scale for assessing depression and the quality of life of EQ-5D, and the subjective effectiveness of therapy by patients and doctors was evaluated. Results: Combination therapy resulted in significantly greater regression of cognitive impairment compared to monotherapy. At the end of the study, the differences between the groups were significant both on the MMSE scale (p=0.007) and on the MoCA scale (p=00003). At the same time, significant differences between the groups in the magnitude of cognitive improvement on the MoCA scale were noted already from the 30th day of treatment. Combination therapy also contributed to a more significant improvement in the patient's quality of life: dynamics on the EQ-5D scale significantly (p<0.05) differed in the groups, also starting from the 30th day of therapy. There were no significant differences in the dynamics of the Hamilton scale for assessing depression between the compared groups. Both Picamilon Ginkgo and monotherapy with ginkgo biloba extract were safe and were not accompanied by significant adverse events. Conclusion: The combination of standardized ginkgo biloba extract with Picamilon has an advantage over monotherapy with ginkgo biloba extract in patients with chronic cerebral ischemia, as it contributes to a more significant regression of cognitive impairment and improvement of quality of life.
[Effects of aminalon, fenibut, and Picamilon on the typological parameters of cerebral hemodynamics in swimmers with dysadaptation syndrome]
Eksp Klin Farmakol 2009 Jul-Aug;72(4):15-9.PMID:19803364doi
The administration of aminalon (0.25 g), fenibut (0.25 g) and Picamilon (0.10 g) during 4 weeks as a means of recovery for swimmers with disadaptation syndrome helped to optimize the biochemical status and cerebral circulation 20-min after warm-up. The reaction to the warm-up load under test conditions was characterized by increasing total blood filling of the brain and difficulty of venous outflow. Under the action of drugs, a decrease in blood filling of the brain and increase in venous blood outflow from the cerebral basin was observed 20 min after load in all test groups (except the hypokinetic group taking Picamilon).