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GT 2016 is a 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.
| Molecular Weight | 317.47 |
| Formula | C19H31N3O |
| CAS Number | 152241-24-2 |
| Solubility (25°C) | DMSO 31.75 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Lee, et al. Chembiochem. A small-molecule antagonist of the hedgehog signaling pathway.
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