| Stereochemistry | ABSOLUTE |
| Molecular Formula | C11H16N2O |
| Molecular Weight | 192.2575 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(OC[C@@H]2CCCN2)C=CC=N1
InChI
InChIKey=YRVIKLBSVVNSHF-JTQLQIEISA-N
InChI=1S/C11H16N2O/c1-9-11(5-3-6-12-9)14-8-10-4-2-7-13-10/h3,5-6,10,13H,2,4,7-8H2,1H3/t10-/m0/s1
Pozanicline is an alpha4-beta2 neuronal nicotinic receptor partial agonist. It had been in phase II clinical trials for the treatment of attention hyperactivity disorder and Alzheimer’s disease. It was tested for the treatment of schizophrenia too. All these studies were discontinued. Modulation of hippocampal learning and memory using Pozanicline in animal model was effective as novel therapeutic strategies for nicotine addiction. However future clinical trial was terminated.
CNS Activity
Originator
Approval Year
Doses
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as victim
Tox targets
PubMed
Sample Use Guides
No significant stimulation was observed for Pozanicline concentrations between 1 uM and 300 uM on [3H]-ACh release from mouse interpeduncular nucleus synaptosomes indicating no agonist activity in this concentration range. Subsequently the inhibitory activity of Pozanicline on nicotine-stimulated [3H]-ACh release from mouse interpeduncular nucleus synaptosomes was tested. No inhibition of [3H]-ACh release stimulated by 30 uM nicotine was observed for simultaneous exposure of the synaptosomes to nicotine and concentrations of Pozanicline between 1 uM and 300 uM. However, inhibition was observed when the concentration of Pozanicline was increased to 1000 uM.
ACTIVE MOIETY
SALT/SOLVATE (PARENT)
