Stereochemistry | ACHIRAL |
Molecular Formula | C23H24FN3O2S |
Molecular Weight | 425.519 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=CC=C(C=C1)N2CCN(CCCN3C4=CC=CC5=C4C(=CC=C5)S3(=O)=O)CC2
InChI
InChIKey=VGIGHGMPMUCLIQ-UHFFFAOYSA-N
InChI=1S/C23H24FN3O2S/c24-19-8-10-20(11-9-19)26-16-14-25(15-17-26)12-3-13-27-21-6-1-4-18-5-2-7-22(23(18)21)30(27,28)29/h1-2,4-11H,3,12-17H2
Fananserin is a potential antipsychotic compound with a high affinity for both D4 and 5-HT2A receptors, and negligible affinity for D2 receptors. Fananserin has been researched for the treatment of schizophrenia. Fananserin was the first selective D4/5-HT2A antagonist to undergo clinical trials for schizophrenia. It has a high affinity for D4 (Ki 2.9 nM) and 5-HT2A (Ki 0.37 nM) receptors and is over 100-fold selective versus H1, a1 adrenergic, 5-HT1A and D2 dopamine receptors. Development of this compound was halted following
phase II clinical trials due to lack of efficacy.
CNS Activity
Originator
Approval Year
Sourcing
PubMed
Patents
Sample Use Guides
Treatment of schizophrenia: doses of fananserin reached 250 mg b.i.d. over 28 days, starting with an 8-day escalation.
Route of Administration:
Oral