Endomorphin-1
(Synonyms: 内吗啡肽 1) 目录号 : GP10065
An endogenous neuropeptide and μ-opioid receptor agonist
Cas No.:189388-22-5
Sample solution is provided at 25 µL, 10mM.
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Endomorphins are two endogenous opioid peptides. Endomorphin-1 (Tyr-Pro-Trp-Phe-NH2) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH2) are tetrapeptides with the highest known affinity and specificity for the μ opioid receptor. Endomorphin-1 is located in the nucleus of the solitary tract, the periventricular hypothalamus, and the dorsomedial hypothalamus, where it is found within histaminergic neurons and may regulate sedative and arousal behaviors1. It is assumed that endomorphins are the cleavage products of a larger precursor, but this polypeptide or protein has not yet been identified. Perikarya expressing EM2-like immunoreactivity were present in the posterior hypothalamus, whereas those expressing EM1-like immunoreactivity were present in both the posterior hypothalamus and the nucleus of the solitary tract (NTS). EM1-like immunoreactivity was more widely and densely distributed throughout the brain than was EM2-like immunoreactivity, whereas EM2-like immunoreactivity was more prevalent in the spinal cord than was EM1-like immunoreactivity. endomorphins participate in modulating nociceptive and autonomic nervous system processes and responsiveness to stress.
References:
1. Greco, MA; Fuller, PM; Jhou, TC; Martin-Schild, S; Zadina, JE; Hu, Z; Shiromani, P; Lu, J (2008). "Opioidergic projections to sleep-active neurons in the ventrolateral preoptic nucleus". Brain Research 1245: 96–107.
| Cell experiment [1]: | |
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Cell lines |
Primary human fetal mixed glial/neuronal brain cell, human microglial cell |
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Preparation method |
The solubility of this compound in DMSO is >30.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1 nM |
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Applications |
In mixed glial/neuronal cell cultures infected with HIV-1, endomorphin-1 potentiated the expression of HIV-1 in a bell-shaped dose-response manner. Endomorphin-1 (0.1 nM) consistently amplified the replication of HIV-1. In microglial cells, endomorphin-1 potentiated the expression of HIV-1, with maximal enhancement of HIV-1 expression at 10-10M. |
| Animal experiment [2, 3]: | |
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Animal models |
Male ICR mice, adult female Sprague–Dawley rats |
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Dosage form |
i.c.v. injection, 5 min, 3.28 nM-16.38 nM, intrathecal injection |
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Application |
Endomorphin-1 inhibited the tail-flick (AD50 = 6.16 nM) and hot-plate responses (AD50 = 1.94 nM) in a dose-dependent manner at 5 min after i.c.v. injection. In rats, intrathecal injection of 1:10 and 1:100 times diluted EM1 antiserum significantly decreased the effect of 2 Hz electroacupuncture analgesia. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Peterson P K, Gekker G, Hu S, et al. Endomorphin-1 potentiates HIV-1 expression in human brain cell cultures: implication of an atypical μ-opoid receptor[J]. Neuropharmacology, 1999, 38(2): 273-278. [2]. Tseng L F, Narita M, Suganuma C, et al. Differential antinociceptive effects of endomorphin-1 and endomorphin-2 in the mouse[J]. Journal of Pharmacology and Experimental Therapeutics, 2000, 292(2): 576-583. [3]. Han Z, Jiang Y H, Wan Y, et al. Endomorphin-1 mediates 2 Hz but not 100 Hz electroacupuncture analgesia in the rat[J]. Neuroscience letters, 1999, 274(2): 75-78. | |
| Cas No. | 189388-22-5 | SDF | |
| 别名 | 内吗啡肽 1 | ||
| 化学名 | (2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pyrrolidine-2-carboxamide | ||
| Canonical SMILES | C1CC(N(C1)C(=O)C(CC2=CC=C(C=C2)O)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC5=CC=CC=C5)C(=O)N | ||
| 分子式 | C34H38N6O5 | 分子量 | 610.67 |
| 溶解度 | ≥ 30.55mg/mL in DMSO | 储存条件 | Desiccate 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 | 1.6375 mL | 8.1877 mL | 16.3755 mL |
| 5 mM | 0.3275 mL | 1.6375 mL | 3.2751 mL |
| 10 mM | 0.1638 mL | 0.8188 mL | 1.6375 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet