CPCCOEt |
Catalog No.GC18134
One-Click Copy Product Info
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CPCCOEt is a non-competitive metabotropic glutamate receptor 1 (mGluR1) antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 179067-99-3
Sample solution is provided at 25 µL, 10mM.
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CPCCOEt is a non-competitive metabotropic glutamate receptor 1 (mGluR1) antagonist. CPCCOEt inhibits receptor signaling by binding to the transmembrane domain of mGluR1, disrupting the intramolecular interaction between the agonist-bound extracellular domain and the transmembrane domain. CPCCOEt can be used in neuroscience and oncology-related research[1-4].
In vitro, Hs683, A172, and U87 glioma cell lines were treated with CPCCOEt (100-350μM) for five days. CPCCOEt significantly reduced the viability of these cells in a concentration-dependent manner[5]. CHO cells expressing the human mGlu1a receptor were pretreated with CPCCOEt (3μM–300μM) for 30 minutes, followed by stimulation with L-quisqualate (10μM) for 30 minutes. CPCCOEt significantly inhibited L-quisqualate-induced phosphoinositide hydrolysis and reduced mGlu1a receptor-mediated signaling[6].
In vivo, CPCCOEt (500nmoles; single treatment) was administered via intrathecal injection to chronic constriction injury rats 20 minutes before formalin stimulation. CPCCOEt significantly reduced formalin-induced nociception in CCI rats, as well as the associated increases in spinal glutamate concentrations[7]. In male C57BL/6J mice (10-24 weeks old), CPCCOEt (10 and 30mg/kg; single treatment) was administered via intraperitoneal injection 10 minutes before ethanol (4.0g/kg) administration. CPCCOEt did not significantly alter ethanol-induced sedation and hypnotic effects[8].
References:
[1] Litschig S, Gasparini F, Rueegg D, et al. CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding. Mol Pharmacol. 1999 Mar;55(3):453-61.
[2] Bräuner-Osborne H, Jensen AA, Krogsgaard-Larsen P. Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor. Neuroreport. 1999 Dec 16;10(18):3923-5.
[3] Fukunaga I, Yeo CH, Batchelor AM. The mGlu1 antagonist CPCCOEt enhances the climbing fibre response in Purkinje neurones independently of glutamate receptors. Neuropharmacology. 2007 Feb;52(2):450-8.
[4] Haas HS, Pfragner R, Siegl V, et al. The non-competitive metabotropic glutamate receptor-1 antagonist CPCCOEt inhibits the in vitro growth of human melanoma. Oncol Rep. 2007 Jun;17(6):1399-404.
[5] Dalley CB, Wroblewska B, Wolfe BB, et al. The Role of Metabotropic Glutamate Receptor 1 Dependent Signaling in Glioma Viability. J Pharmacol Exp Ther. 2018 Oct;367(1):59-70.
[6] Hermans E, Nahorski SR, Challiss RA. Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1alpha metabotropic glutamate receptor. Neuropharmacology. 1998 Dec;37(12):1645-7.
[7] Kumar N, Laferriere A, Yu JS, et al. Metabotropic glutamate receptors (mGluRs) regulate noxious stimulus-induced glutamate release in the spinal cord dorsal horn of rats with neuropathic and inflammatory pain. J Neurochem. 2010 Jul;114(1):281-90.
[8] Sharko AC, Hodge CW. Differential modulation of ethanol-induced sedation and hypnosis by metabotropic glutamate receptor antagonists in C57BL/6J mice. Alcohol Clin Exp Res. 2008 Jan;32(1):67-76.
| Cell experiment [1]: | |
Cell lines | CHO cells expressing the human metabotropic glutamate receptor mGlu1a (CHO-Lac-mGlu1α) |
Preparation Method | CHO cells were seeded into 24-well multidishes in the presence of 1μCi/ml myo-[³H]inositol 48 hours before agonist/antagonist manipulation. During the last 20 hours of culture, 100μM isopropyl-β-D-thiogalactoside (IPTG) was added to the culture medium to induce mGlu1a receptor expression. The cell monolayers were washed with Krebs-Henseleit buffer. All experiments were performed in the presence of 3U/ml glutamic-pyruvic transaminase and 3mM pyruvate to prevent receptor activation by endogenous glutamate. CPCCOEt (3μM–300μM) was added 30 minutes before, and LiCl (10mM) 15 minutes before the addition of the agonist L-quisqualate (10μM). Stimulation with the agonist lasted for 30 minutes. |
Reaction Conditions | 3μM–300μM; 30min |
Applications | CPCCOEt antagonized L-quisqualate-induced phosphoinositide hydrolysis in a non-competitive and reversible manner. CPCCOEt significantly inhibited L-quisqualate-stimulated [³H]InsP accumulation, with complete inhibition of mGlu1a receptor-mediated signalling observed in the presence of 300μM CPCCOEt. |
| Animal experiment [2]: | |
Animal models | Male Long Evans hooded rats with chronic constriction injury (CCI) of the sciatic nerve or hind paw injection of complete Freund's adjuvant (CFA) |
Preparation Method | Rats were implanted with a chronic indwelling intrathecal (i.t.) catheter. For behavioral testing, rats were placed in an observation chamber for a 30-40 minute habituation period. Rats were then lightly anesthetized with isofluorane for an intrathecal injection of CPCCOEt or vehicle, and returned to the chamber. Post-injection measurements began 20 minutes after injection. Sustained nociceptive behaviors were recorded following a subcutaneous (s.c.) injection of 1.0% formalin (for CCI rats) or 0.03% capsaicin (for CFA rats) into the ipsilateral plantar hind paw. |
Dosage form | 500nmoles; i.t.; single injection |
Applications | CPCCOEt significantly reduced formalin-induced nociception in CCI rats and capsaicin-induced nociception in CFA rats. CPCCOEt significantly attenuated the formalin-induced increases in spinal glutamate concentrations in CCI rats and the capsaicin-induced increases in spinal glutamate concentrations in CFA rats. |
References: | |
| Cas No. | 179067-99-3 | SDF | |
| Chemical Name | (1aS,7aS,Z)-ethyl 7-(hydroxyimino)-1,1a,7,7a-tetrahydrocyclopropa[b]chromene-1a-carboxylate | ||
| Canonical SMILES | O=C([C@]1([C@H]/2C1)OC3=CC=CC=C3C2=N/O)OCC | ||
| Formula | C13H13NO4 | M.Wt | 247.25 |
| Solubility | DMSO: 100 mM | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0445 mL | 20.2224 mL | 40.4449 mL |
| 5 mM | 808.9 μL | 4.0445 mL | 8.089 mL |
| 10 mM | 404.4 μL | 2.0222 mL | 4.0445 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)