| CAS NO: | 78123-71-4 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | White lyophilised solid |
| Storage | Desiccate at -20°C |
| M.Wt | 513.7 |
| Cas No. | 78123-71-4 |
| Formula | C26H35N5O6 |
| Solubility | ≥40.7 mg/mL in EtOH; ≥40.7 mg/mL in H2O; ≥42.2 mg/mL in DMSO |
| Chemical Name | (S)-2-amino-N-((R)-1-((2-(((S)-1-((2-hydroxyethyl)amino)-1-oxo-3-phenylpropan-2-yl)(methyl)amino)-2-oxoethyl)amino)-1-oxopropan-2-yl)-3-(4-hydroxyphenyl)propanamide |
| Canonical SMILES | O=C([C@H](CC1=CC=CC=C1)N(C)C(CNC([C@@H](C)NC([C@H](CC(C=C2)=CC=C2O)N)=O)=O)=O)NCCO |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 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。溶液形式一般不宜长期储存，请尽快用完。 |
DAMGO is a selective peptide agonist of the μ-opioid receptor (Ki = 1.18, 1430, and 213 nM for human μ-, δ-, and κ-opioid receptors, respectively) [1].
Opioid receptors are members of the class A family of G protein-coupled receptors (GPCRs), which transduce signals via heterotrimeric G proteins on the inner surface of the plasma membrane, leading to intracellular signaling cascades involved in many aspects of cellular function. Four opioid receptor types exist [μ, δ, κ, and opioid receptor-like 1 (ORL1)], among which the μ-opioid receptor has been most explored as its agonists are used to treat chronic pain [2].
In C6μ cell membranes, DAMGO at 10 μM produced a 250% stimulation of [35S]GTPγS binding above basal activity through the μ-opioid receptors, with an EC50 of 222 nM [2]. In mousevas deferens (MVD), DAMGO strongly inhibited the electrically-evoked MVD muscle contractions in concentration dependent manner, with EC50 value of 238.47 nM [3].
In the rat late permanent visceral pain model, DAMGO produced dose-dependent antinociceptive action, with potency similar to that of morphine when given i.p. to the same site where acetic acid was injected. The calculated ED50 values were 238.57 nmol/kg for morphine and 289.52 nmol/kg for DAMGO [4].
References:
[1]. Zhao G M, Qian X, Schiller P W, et al. Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at μ, δ, and κ opioid receptors. Journal of Pharmacology and Experimental Therapeutics, 2003, 307(3): 947-954.
[2]. Burford N T, Clark M J, Wehrman T S, et al. Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor. Proceedings of the National Academy of Sciences of the United States of America, 2013, 110(26): 10830-10835.
[3]. Lacko E, Varadi A, Rapavi R, et al. A novel μ-opioid receptor ligand with high in vitro and in vivo agonist efficacy. Current Medicinal Chemistry, 2012, 19(27): 4699-4707.
[4]. Al-Khrasani M, Lackó E, Riba P, et al. The central versus peripheral antinociceptive effects of μ-opioid receptor agonists in the new model of rat visceral pain. Brain Research Bulletin, 2012, 87(2-3): 238-243.
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