Details
| 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
SMILES
C(C1=CC=CC=C1)C2=NC=C3CCNCCC3=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
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.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21195614 | http://adisinsight.springer.com/drugs/800023681
Curator's Comment: # Pfizer
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. | 2011 May 1 |
|
| Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists. | 2015 Mar 12 |
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
In Vitro Use Guide
Curator's Comment: Pharmacological evaluation for activity at the 5-HT2A receptor
was measured in a FLIPR assay employing Swiss 3T3 cells expressing
the recombinant human 5-HT2A receptor
Screening
of PF-3246799 in the 5-HT2A recombinant assay gave a significant response
with an EC50 68 nM and Emax 82%. PF-3246799 showed weak but measurable agonism of 5-HT2B
at 10 uM in both recombinant cell systems and native
human tissue.
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SUBSTANCE RECORD
![Structure of 2-Benzyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepine](/img/fef763c7-b89f-4cc1-a43c-e791d1a3f8bb.svg "Structure of 2-Benzyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepine")