| Stereochemistry | ACHIRAL |
| Molecular Formula | C15H17N3 |
| Molecular Weight | 239.3156 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
![Structure of 2-Benzyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepine](/img/8fe50081-e2c3-44e9-af12-a5e53c6d0eb6.svg?size=400&version=5&stereo=false "Structure of 2-Benzyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepine")
SMILES
C(C1=CC=CC=C1)C2=NC3=C(CCNCC3)C=N2
InChI
InChIKey=CZWQBSKNHUVZLI-UHFFFAOYSA-N
InChI=1S/C15H17N3/c1-2-4-12(5-3-1)10-15-17-11-13-6-8-16-9-7-14(13)18-15/h1-5,11,16H,6-10H2
| Molecular Formula | C15H17N3 |
| Molecular Weight | 239.3156 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
PF-03246799 (PF-3246799) is a potent 5-HT2C receptor agonist. PF-3246799 had
minimal activation at either the 5-HT2A or 5-HT2B receptors, combined
with robust efficacy in a preclinical canine model of SUI and
attractive pharmacokinetic and safety properties. It is a candidate for clinical development for the treatment of SUI.
CNS Activity
Originator
Approval Year
PubMed
Sample Use Guides
Rats: Following single intravenous administration (1 mg/kg) of PF-3246799
to rat, plasma clearance was moderate relative to liver blood flow
and volume of distribution was moderate resulting in an elimination
half-life of 2.8 h.
Following single oral administration to rat (2 mg/kg), PF-3246799 was rapidly
absorbed and showed moderate oral bioavailability (40%) suggesting
complete absorption from the gut, based on blood clearance of
51 ml/min/kg and an assumed liver blood flow of 70 ml/min/kg.
Dogs: Following single
intravenous administration to dog (0.030 mg/kg), plasma clearance of PF-3246799 was
low relative to liver blood flow resulting in an elimination half-life
of 3.4 h.
Route of Administration:
Other