GT-2016 is a potent, selective, and brain-penetrant histamine H₃ receptor antagonist with a Ki of 43.8 nM, exhibiting high selectivity over H₁ and H₂ receptors (IC₅₀ >10 μM) and no activity against histamine methyltransferase at concentrations up to 3 μM. By antagonizing presynaptic H₃ autoreceptors, GT-2016 enhances histamine release in the cerebral cortex, increasing extracellular histamine levels by approximately 75% in rat models within one hour of administration. Originally developed by Gliatech, Inc., for potential treatment of neurological disorders such as Alzheimer's disease, GT-2016's development was eventually discontinued.
MedKoo Cat#: 573568
Name: GT-2016
CAS#: 152241-24-2
Chemical Formula: C19H31N3O
Exact Mass: 317.2467
Molecular Weight: 317.48
Elemental Analysis: C, 71.88; H, 9.84; N, 13.24; O, 5.04
The following data is based on the product molecular weight 317.48 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 |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
