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说明： Potent and selective μ antagonist
纯度： ≥95% (HPLC)
生物活性 for CTAP
CTAP is a potent and selective μ opioid receptor antagonist (IC50 = 3.5 nM). Displays > 1200-fold selectivity over δ opioid and somatostatin receptors. Brain penetrant and active in vivo.
技术数据 for CTAP
| 分子量 | 1104.32 |
| 公式 | C51H69N13O11S2 |
| 序列 |
FCYWRTXT (Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X = Pen, Disulfide bridge: 2-7, Thr-8 = C-terminal amide) |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 103429-32-9 |
| PubChem ID | 90479802 |
| InChI Key | OFMQLVRLOGHAJI-KOFBULAQSA-N |
| Smiles | [H]N[C@H](CC1=CC=CC=C1)C(=O)N[C@H]1CSSC(C)(C)C(NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC1=O)[C@@H](C)O)C(=O)N[C@@H]([C@@H](C)O)C(N)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for CTAP
| 溶解性 | Soluble to 1 mg/ml in water |
产品说明书 for CTAP
参考文献 for CTAP
参考文献是支持产品生物活性的出版物。
Abbruscato et al (1997) Blood-brain barrier permeability and bioavailability of a highly potent and μ-selective opioid receptor antagonist, CTAP: comparison with mor. J.Pharmacol.Exp.Ther. 280 402 PMID: 8996221
Kramer et al (1989) Novel peptidic mu opioid antagonists: pharmacologic characterization in vitro and in vivo. J.Pharmacol.Exp.Ther. 249 544 PMID: 2566679
Pelton et al (1986) Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for μ opioid receptors. J.Med.Chem. 29 2370 PMID: 2878079
If you know of a relevant reference for CTAP, please let us know.
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关键词: CTAP, CTAP supplier, Selective, potent, μ-opioid, mu-opioid, antagonists, MOP, Receptors, OP3, Mu, Opioid, 1560, Tocris Bioscience
13 篇 CTAP 的引用文献
引用文献是使用了 Tocris 产品的出版物。 CTAP 的部分引用包括：
Fox and Hentges (2017) Differential Desensitization Observed at Multiple Effectors of Somatic μ-Opioid Receptors Underlies Sustained Agonist-Mediated Inhibition of Proopiomelanocortin Neuron Activity. J Neurosci 37 8667 PMID: 28821664
Gerhold et al (2015) Pronociceptive and Antinociceptive Effects of Bupren. in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude. J Neurosci 35 9580 PMID: 26134641
Song et al (2011) Protein kinase Czeta mediates micro-opioid receptor-induced cross-desensitization of chemokine receptor CCR5. J Biol Chem 286 20354 PMID: 21454526
Krook-Magnuson et al (2011) Ivy and neurogliaform interneurons are a major target of μ-opioid receptor modulation. J Neurosci 31 14861 PMID: 22016519
Happel et al (2008) DAMGO-induced expression of chemokines and chemokine receptors: the role of TGF-β1. Front Cell Neurosci 83 956 PMID: 18252865
Sengupta et al (2009) Morphine increases brain levels of ferritin heavy chain leading to inhibition of CXCR4-mediated survival signaling in neurons. J Leukoc Biol 29 2534 PMID: 19244528
Nash et al (2019) MOR-Induced Modulation of Endolysosomal Iron Mediates Upregulation of Ferritin Heavy Chain in Cortical Neurons. Eneuro 6 PMID: 31300544
Maguma et al (2012) Differences in the characteristics of tolerance to μ-opioid receptor agonists in the colon from wild type and β-arrestin2 knockout mice. Eur J Pharmacol 685 133 PMID: 22521552
Pennock et al (2012) Multiple inhibitory G-protein-coupled receptors resist acute desensitization in the presynaptic but not postsynaptic compartments of neurons. J Neurosci 32 10192 PMID: 22836254
Birdsong et al (2019) Synapse-specific opioid modulation of thalamo-cortico-striatal circuits. Elife 8 PMID: 31099753
Largent-Milnes et al (2013) Building a better analgesic: multifunctional compounds that address injury-induced pathology to enhance analgesic efficacy while eliminating unwanted side effects. J Pharmacol Exp Ther 347 7 PMID: 23860305
Milan-Lobo et al (2013) Anti-analgesic effect of the mu/delta opioid receptor heteromer revealed by ligand-biased antagonism. PLoS One 8 e58362 PMID: 23554887
DiPatrizio (2008) Activating parabrachial cannabinoid CB1 receptors selectively stimulates feeding of palatable foods in rats. J Neurosci 28 9702 PMID: 18815256
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