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Description: Potent and selective μ antagonist
Purity: ≥95% (HPLC)
Citations (13)
Literature (2)

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

M. Wt 1104.32
Formula C51H69N13O11S2

(Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X = Pen, Disulfide bridge: 2-7, Thr-8 = C-terminal amide)

Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 103429-32-9
PubChem ID 90479802
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

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

Product Datasheets for CTAP

Certificate of Analysis / Product Datasheet
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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:

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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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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

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