Biological Activity
Positive allosteric modulator of GABAA receptors. Enhances GABA-induced Cl- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. Causes sedation in vivo following i.v. administration without losing "righting reflex". Also displays antioxidant activity.
Technical Data
| M. Wt | 321.85 |
| Formula | C16H23N5.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 157013-85-9 |
| PubChem ID | 56972182 |
| InChI Key | MNKBXPNQWKUSKU-UHFFFAOYSA-N |
| Smiles | CC2=CC1=C(N3CCCC3)N=C(N4CCCC4)N=C1N2C.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 16.09 | 50 | |
| water | 8.05 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 321.85. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.11 mL | 15.54 mL | 31.07 mL |
| 5 mM | 0.62 mL | 3.11 mL | 6.21 mL |
| 10 mM | 0.31 mL | 1.55 mL | 3.11 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.62 mL |
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References
References are publications that support the products' biological activity.
Bundy et al (1995) Synthesis of novel 2,4-diaminopyrrolo-[2,3-d]pyrimidines with antioxidant, neuroprotective, and antiasthma activity. J.Med.Chem. 38 4161 PMID: 7473542
Haesook et al (1995) U-89843A is a novel allosteric modulator of γ-aminobutyric acidA receptors. J.Pharmacol.Exp.Ther. 275 1390 PMID: 8531107
Rohn et al (1996) Inhibition of Ca2+-pump ATPase and the Na+/K+-pump ATPase by iron-generated free radicals. Biochem.Pharmacol. 51 471 PMID: 8619892
Keywords: U 89843A, supplier, Positive, allosteric, modulators, GABAA, receptors, Receptors, U89843A, PNU89843, PNU, 89843, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
