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Biological Activity 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.
Technical Data for CTAP
(Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X = Pen, Disulfide bridge between 2 - 7, Thr-8 = C-terminal amide)
|Storage||Desiccate at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CTAP
|Solubility||Soluble to 1 mg/ml in water|
References for CTAP
References are publications that support the biological activity of the product.
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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Keywords: CTAP, CTAP supplier, Selective, potent, μ-opioid, mu-opioid, antagonists, MOP, Receptors, OP3, Mu, Opioid, 1560, Tocris Bioscience
13 Citations for CTAP
Citations are publications that use Tocris products. Selected citations for CTAP include:
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
Birdsong et al (2019) Synapse-specific opioid modulation of thalamo-cortico-striatal circuits. Elife 8 PMID: 31099753
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
Nash et al (2019) MOR-Induced Modulation of Endolysosomal Iron Mediates Upregulation of Ferritin Heavy Chain in Cortical Neurons. Eneuro 6 PMID: 31300544
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
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
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
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
DiPatrizio (2008) Activating parabrachial cannabinoid CB1 receptors selectively stimulates feeding of palatable foods in rats. J Neurosci 28 9702 PMID: 18815256
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
Do you know of a great paper that uses CTAP from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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