Endomorphin-2
(Synonyms: 内吗啡肽 2) 目录号 : GC10059
Endomorphin-2是一种高亲和力、高选择性的μ-阿片受体激动剂（Ki = 0.69nM）。
Cas No.:141801-26-5
Sample solution is provided at 25 µL, 10mM.
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Endomorphin-2 is a high-affinity and highly selective agonist of the μ-opioid receptor (Ki = 0.69nM) [1]. Endomorphin-2 activates MOR, blocking calcium channels and enhancing potassium channel opening on neurons, thereby inhibiting neural activity and achieving analgesic effects [2-3]. Endomorphin-2 is primarily used in the study of chronic pain [4].
In Wistar rats, intrahypothalamic injection of Endomorphin-2 (0.50-0.75μmol/kg; intrahypothalamic injection; single injection) induced a significant dose-related increase in food intake [5]. In CD1 mice, intraventricular injection of Endomorphin-2 (0.3-30μg; 10μL; intraventricular injection; single injection) can dose-dependently shorten the immobility time of animals in the TST test [6].
References:
[1]. Dvoracsko S, Stefanucci A, Novellino E, et al. The design of multitarget ligands for chronic and neuropathic pain[J]. Future medicinal chemistry, 2015, 7(18): 2469-2483.
[2]. Horvath G. Endomorphin-1 and endomorphin-2: pharmacology of the selective endogenous μ-opioid receptor agonists[J]. Pharmacology & therapeutics, 2000, 88(3): 437-463.
[3]. Chen Y B, Huang F S, Fen B, et al. Inhibitory effects of endomorphin-2 on excitatory synaptic transmission and the neuronal excitability of sacral parasympathetic preganglionic neurons in young rats[J]. Frontiers in cellular neuroscience, 2015, 9: 206.
[4]. Wolfe D, Hao S, Hu J, et al. Engineering an endomorphin-2 gene for use in neuropathic pain therapy[J]. PAIN®, 2007, 133(1-3): 29-38.
[5]. Brunetti L, Ferrante C, Orlando G, et al. Orexigenic effects of endomorphin-2 (EM-2) related to decreased CRH gene expression and increased dopamine and norepinephrine activity in the hypothalamus[J]. Peptides, 2013, 48: 83-88.
[6]. Fichna J, Janecka A, Piestrzeniewicz M, et al. Antidepressant-like effect of endomorphin-1 and endomorphin-2 in mice[J]. Neuropsychopharmacology, 2007, 32(4): 813-821.
Endomorphin-2是一种高亲和力、高选择性的μ-阿片受体激动剂（Ki = 0.69nM） [1]。Endomorphin-2激活MOR，阻断钙通道并增强神经元钾通道开放，从而抑制神经活动并达到镇痛作用 [2-3]。Endomorphin-2主要用于慢性疼痛的研究 [4]。
在Wistar大鼠中，下丘脑注射Endomorphin-2（0.50-0.75μmol/kg；下丘脑注射；单次注射）可显著增加大鼠的食物摄入量 [5]。在CD1小鼠中，脑室内注射Endomorphin-2（0.3-30μg；10μL；脑室内注射；单次注射）可剂量依赖性地缩短动物在TST试验中的静止时间 [6]。
| Animal experiment [1]: | |
Animal models | Wistar rats |
Preparation Method | Sixty-four rats were anesthetized with chloral hydrate (400mg/kg, i.p.), treated with ketoprofen (1.4mg/kg), and fixed in a stereotaxic apparatus. After midline incision and local lidocaine (2%), a 21-gauge stainless steel cannula (1.7cm) was implanted into the arcuate nucleus (ARC; AP −3mm from bregma, DV −7mm) and secured with screws and dental cement. A sterile obturator was used to prevent occlusion. Postoperatively, rats received s.c. saline (1mL), 5% glucose (1mL), and piperacillin (30mg/kg, i.p.) and were monitored for 72h until recovery. At 72h, 10µL of drug/vehicle was microinjected into the ARC at 9:00 AM: Endomorphin-2 (0.50–0.75µmol/kg) or Endomorphin-2 (0.50µmol/kg) plus β-funaltrexamine (0.20µmol/kg). Injections were performed via a 10µL syringe connected to the cannula. |
Dosage form | 0.50-0.75μmol/kg; intrahypothalamic injection; single injection |
Applications | Compared to vehicle, intrahypothalamic injection of Endomorphin-2 induced a significant dose-related increase in food intake, as evaluated 24h after treatment. |
References: | |
| Cas No. | 141801-26-5 | SDF | |
| 别名 | 内吗啡肽 2 | ||
| 化学名 | (S)-N-((S)-1-(((S)-1-amino-1-oxo-3-phenylpropan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)-1-((S)-2-amino-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide | ||
| Canonical SMILES | O=C([C@H]1N(C([C@H](CC(C=C2)=CC=C2O)N)=O)CCC1)N[C@H](C(N[C@H](C(N)=O)CC3=CC=CC=C3)=O)CC4=CC=CC=C4 | ||
| 分子式 | C32H37N5O5 | 分子量 | 571.65 |
| 溶解度 | ≥ 57.2mg/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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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7493 mL | 8.7466 mL | 17.4932 mL |
| 5 mM | 349.9 μL | 1.7493 mL | 3.4986 mL |
| 10 mM | 174.9 μL | 874.7 μL | 1.7493 mL |
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| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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，
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2.
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Quality Control & SDS
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- Purity: >98.00%
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