| Stereochemistry | RACEMIC |
| Molecular Formula | C16H24N2O2 |
| Molecular Weight | 276.374 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC1=C(C)NC2=C1C(=O)C(CN3CCOCC3)CC2
InChI
InChIKey=KLPWJLBORRMFGK-UHFFFAOYSA-N
InChI=1S/C16H24N2O2/c1-3-13-11(2)17-14-5-4-12(16(19)15(13)14)10-18-6-8-20-9-7-18/h12,17H,3-10H2,1-2H3
Molindone (Moban) is a therapeutic antipsychotic, used in the treatment of schizophrenia. The exact mechanism has not been established, however, based on electroencephalogram (EEG) studies, molindone is thought to act by occupying (antagonizing) dopamine (D2) receptor sites in the reticular limbic systems in the brain, thus decreasing dopamine activity. Decreased dopamine activity results in decreased physiological effects normally induced by excessive dopamine stimulation, such as those typically seen in manifestations of psychotic disorders. The side effect profile of molindone is similar to that of other typical antipsychotics. Unlike most antipsychotics, however, molindone use is associated with weight loss.
CNS Activity
Originator
Approval Year
Doses
AEs
Sourcing
PubMed
Patents
Sample Use Guides
Initial Dosage Schedule The usual starting dosage is 50-75 mg/day. Increase to 100 mg/day in 3 or 4 days. Based on severity of symptomatology, dosage may be titrated up or down depending on individual patient response. An increase to 225 mg/day may be required in patients with severe symptomatology. Elderly and debilitated patients should be started on lower dosage.
Maintenance Dosage Schedule Mild-5 mg-15 mg three or four times a day. Moderate-10 mg-25 mg three or four times a day. Severe-225 mg/day may be required.
Route of Administration:
Oral
Salmonella typhimurium tester strains TA98, TA100, TA1535, TA1537 were used for Genotoxicity evaluation. S9 homogenates were added into a “mix” at a final concentration of 10% and the mix was supplemented with GSH (30 mM) and UDPGA (trisodium salt; 15 mM) as needed. The components of the S9 “mix” (per mL) included 0.7 mL water, 0.10 mL of 1M NaH2PO4/Na2HPO4 (pH 7.4), 0.02 mL of 0.25M glucose-6-phosphate, 0.04 mL of NADP, 0.04 mL of 0.825M KCl/0.2M MgCl2 and 0.1 mL of S9 homogenate. For the plate incorporation assay without S9, 100 mkL of tester strain and 50 mkL of vehicle control or test substance dilution were added to 2.5 mL of molten selective top agar (maintained at 45+/-2C). When S9 mix was required, 500 mkL of S9 mix, 100 mkL of tester strain and 50 mkL of vehicle control or Molindone dilution were added to 2.0 mL of molten selective agar. The top agar (100 mL) was supplemented with 0.5 mM histidine/biotin for the selection of histidine revertants (Salmonella tester strains) and 0.5 mM of tryptophan for the selection of tryptophan revertants (strain WP2uvrA). After the addition of the required components, the mixture was vortexed and overlaid (in 2.65 mL aliquots) onto the surface of 25 mL of minimal bottom agar contained in a 15 3 100 mm petri dish. Bacterial plates (triplicate plates/concentration/strain for each phase of the assay) were incubated for 5264 h at 378C before counting the revertants. The identification of a positive response was based on at least 2-fold (TA98, TA100, and WP2uvrA) or 3-fold (TA1535 and TA1537) increase in the mean revertants/plate accompanied by a dose-response to increasing concentrations of the Molindone.
ACTIVE MOIETY
SALT/SOLVATE (PARENT)
