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Submit ReviewCGS 12066B dimaleate
Description: 5-HT1B agonist
Chemical Name: 7-Trifluoromethyl-4-(4-methyl-1-piperazinyl)pyrrolo[1,2-a]-quinoxaline dimaleate
Purity: ≥98% (HPLC)
Biological Activity for CGS 12066B dimaleate
CGS 12066B dimaleate is a 5-HT1B full agonist, 10-fold selective over 5-HT1A and 1000-fold selective over 5-HT2C receptors. Centrally active following systemic administration.
Technical Data for CGS 12066B dimaleate
| M. Wt | 566.49 |
| Formula | C17H17F3N4.2C4H4O4 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 109028-10-6 |
| PubChem ID | 9915956 |
| InChI Key | HTEVMLYDEWVIQE-SPIKMXEPSA-N |
| Smiles | O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O.FC(C1=CC3=C(N2C=CC=C2C(N4CCN(CC4)C)=N3)C=C1)(F)F |
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 CGS 12066B dimaleate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 2.83 | 5 | |
| DMSO | 22.66 | 40 |
Preparing Stock Solutions for CGS 12066B dimaleate
The following data is based on the product molecular weight 566.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.4 mM | 4.41 mL | 22.07 mL | 44.13 mL |
| 2 mM | 0.88 mL | 4.41 mL | 8.83 mL |
| 4 mM | 0.44 mL | 2.21 mL | 4.41 mL |
| 20 mM | 0.09 mL | 0.44 mL | 0.88 mL |
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Product Datasheets for CGS 12066B dimaleate
References for CGS 12066B dimaleate
References are publications that support the biological activity of the product.
Neale et al (1987) Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist. Eur.J.Pharmacol. 136 1 PMID: 3496228
Schoeffter and Hoyer (1989) Interaction of arylpiperazines with 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors: do discriminatory 5-HT1B receptor ligands exist? Naunyn Schmiedebergs Arch.Pharmacol. 339 675 PMID: 2770889
Tomkins and O'Neill (2000) Effect of 5-HT1B receptor ligands on self-administration of ethanol in an operant procedure in rats. Pharmacol.Biochem.Behav. 66 129 PMID: 10837852
If you know of a relevant reference for CGS 12066B dimaleate, please let us know.
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Keywords: CGS 12066B dimaleate, CGS 12066B dimaleate supplier, 5-HT1B, agonists, Serotonin, Receptors, 5-HT1, CGS12066B, dimaleate, 0638, Tocris Bioscience
3 Citations for CGS 12066B dimaleate
Citations are publications that use Tocris products. Selected citations for CGS 12066B dimaleate include:
Gadgaard & Jensen (2020) Functional characterization of 5-HT1A and 5-HT1B serotonin receptor signaling through G-protein-activated inwardly rectifying K+ channels in a fluorescence-based membrane potential assay. Biochem Pharmcol 175 PMID: 32088264
Khatri et al (2014) Lasting neurobehavioral abnormalities in rats after neonatal activation of serotonin 1A and 1B receptors: possible mechanisms for serotonin dysfunction in autistic spectrum disorders. Psychopharmacology (Berl) 231 1191 PMID: 23975037
Maciag et al (2006) Evidence that the deficit in sexual behavior in adult rats neonatally exposed to cital. is a consequence of 5-HT1 receptor stimulation during development. Brain Res 1125 171 PMID: 17101120
Do you know of a great paper that uses CGS 12066B dimaleate 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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.