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Endomorphin-1

现货
Catalog No.
A1013
μ阿片类受体高度有效的选择性激动剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
25mg
¥ 490.00
现货

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Background

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 behaviors(1). 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.

A1013_1

FigureFormula of Endomorphin-1

A1013_2

Figure 2  The Endomorphin System and Its Evolving Neurophysiological Role

Ref:

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.

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt610.67
Cas No.189388-22-5
FormulaC34H38N6O5
SynonymsTyr-Pro-Trp-Phe
Solubility≥30.55mg/mL in DMSO
Chemical Name(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
SDFDownload SDF
Canonical SMILESC1CC(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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

原代人胎儿混合胶质细胞/神经元脑细胞,人小胶质细胞

溶解方法

该化合物在DMSO中的溶解度大于30.6 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

0.1 nM

应用

在用HIV-1感染的混合胶质细胞/神经元细胞培养物中,Endomorphin-1以钟形剂量反应方式增强HIV-1的表达。Endomorphin-1(0.1 nM)不断扩大HIV-1的复制。在小胶质细胞中,Endomorphin-1增强了HIV-1的表达,浓度为10-10M时HIV-1表达增加最大。

动物实验 [2, 3]:

动物模型

雄性ICR小鼠,成年雌性Sprague-Dawley大鼠

给药剂量

脑室内注射,5 min,3.28 nM-16.38 nM;鞘内注射

应用

在i.c.v后5分钟,Endomorphin-1以剂量依赖性方式抑制甩尾,AD50为6.16 nM,Endomorphin-1以剂量依赖性方式抑制热板反应,AD50为1.94 nM。在大鼠中,鞘内注射1:10和1:100倍稀释的EM1抗血清显著降低2 Hz电针刺引发的镇痛效果。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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.

质量控制

化学结构

Endomorphin-1