Biological Activity
High affinity H3 receptor antagonist (Ki = 43.8 nM). Displays selectivity against H1 and H2 receptors (IC50 >10 μM). Increases the release of histamine in the cerebral cortex. Displays no activity at histamine methyltransferase in vitro at concentrations up to 3 μM. Brain penetrant.
Technical Data
| M. Wt | 317.47 |
| Formula | C19H31N3O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 152241-24-2 |
| PubChem ID | 9839975 |
| InChI Key | YTCGNPGLMAECND-UHFFFAOYSA-N |
| Smiles | O=C(CCCCC3CCCCC3)N(CC2)CCC2C1=CN=CN1 |
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 | 31.75 | 100 | |
| ethanol | 31.75 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 317.47. 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 | 3.15 mL | 15.75 mL | 31.5 mL |
| 5 mM | 0.63 mL | 3.15 mL | 6.3 mL |
| 10 mM | 0.31 mL | 1.57 mL | 3.15 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.63 mL |
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References
References are publications that support the products' biological activity.
Tedford et al (1995) Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies. J.Pharmacol.Exp.Ther. 275 598 PMID: 7473144
Tedford et al (1999) Development of trans-2-[1H-imidazol-4-yl] cyclopropane derivatives as new high-affinity histamine H3 receptor ligands. J.Pharmacol.Exp.Ther. 289 1160 PMID: 10215700
Yates et al (1999) Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands. J.Pharmacol.Exp.Ther. 289 1151 PMID: 10215699
Keywords: GT 2016, supplier, GT2016, histamine, h3, antagonists, histaminergic, selective, brain, penetrant, centrally, active, Histamine, H3, Receptors, Histamine, H3, Receptors, Tocris Bioscience
