nomifensine
Trade name: Merital
Approved
Jun 1, 1984
Nomifensine, formerly sold under the brand names Merital and Alival, is a norepinephrine–dopamine reuptake inhibitor (NDRI) drug that was developed in the 1960s by Hoechst AG, who then test marketed it in the United States. — Wikipedia
Clinical trial activity
0 trials · 0 clinical orgs · 1 marketing orgs
Timeline
1980s
- Jun 1, 1984
Earliest FDA Approval
Indications
Approved for
Mechanism of action
- Monoamine transporterINHIBITOR
Monoamine transporter inhibitor
It strongly inhibits the re-uptake of dopamine as well as noradrenaline and it is a relatively weak inhibitor of serotonin uptake.
Nomifensine inhibition of norepinephrine (NA) uptake by synaptosomal fractions from rat hypothalamus (IC50 = 7.0 × 10¿7 M) was similar to that of nortriptyline and protriptyline. It was found to be a powerful inhibitor of NA uptake in synaptosomes obtained from whole brain (IC50 = 9.0 × 10¿8 M). Nomifensine had only a moderate effect on serotonin accumulation (IC50 = 2.8 × 10¿5 M).
Approval history
- withdrawnJun 1, 1984
Chemistry & pharmacology
SMILES
CN1Cc2c(N)cccc2C(c2ccccc2)C1- Mol. weight
- 238.33 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL273575 ↗
- WikipediaNomifensine ↗
- NCATS76S8CUH5MR ↗
- ChEMBLCHEMBL1256842 ↗
- ChEMBLCHEMBL1200830 ↗
Also known as
- 2-methyl-4-phenyl-1,2,3,4-tetrahydro-8-isoquinolinamine
- 2-methyl-4-phenyl-1,2,3,4-tetrahydro-8-isoquinolinamine
- 8-amino-1,2,3,4-tetrahydro-2-methyl-4-phenylisochinolin
- 8-amino-1,2,3,4-tetrahydro-2-methyl-4-phenylisochinolin
- 8-amino-1,2,3,4-tetrahydro-2-methyl-4-phenylisoquinoline
- 8-amino-1,2,3,4-tetrahydro-2-methyl-4-phenylisoquinoline
- 8-amino-2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline
- 8-amino-2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline
- hoe-984
- hoe-984
- linamiphen
- merital
- merital
- merital
- merital
- merital
- merital
- merital
- nomifensin
- nomifensin
- nomifensin
- (+-)-nomifensin
- (+-)-nomifensin
- (+/-)-nomifensin
- nomifensina
- nomifensina
- nomifensine
- nomifensine
- nomifensine
- nomifensine
- nomifensine
- nomifensine
- nomifensine
- nomifensine
- (+-)-nomifensine
- (+-)-nomifensine
- (+/-)-nomifensine
- (+)-nomifensine
- (+)-nomifensine
- nomifensine maleate
- nomifensine maleate
- nomifensine maleate
- nomifensinum
- nomifensinum
- (+)-nomiphensine
- (+)-nomiphensine
- (r)-1,2,3,4-tetrahydro-2-methyl-4-phenyl-8-isoquinolinamine
- (r)-1,2,3,4-tetrahydro-2-methyl-4-phenyl-8-isoquinolinamine
Organizations
Marketing (1)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Hoechst | For profit | NDA | — |