General
Preferred name
LOFEPRAMINE
Synonyms
Gamanil ()
Amplit ()
Leo 640 ()
Lopramine ()
LOFEPRAMINE HYDROCHLORIDE ()
Lofepramina ()
WHR-2908A ()
Lomont ()
Lofepramine hcl ()
Feprapax ()
LOFEPRAMINA ()
P&D ID
PD013071
CAS
23047-25-8
26786-32-3
Tags
available
drug
drug candidate
First approval
1977
Drug Status
approved
withdrawn
experimental
investigational
Max Phase
2.0
Drug indication
Major depressive disorder
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Marketed formulations may contain lofepramine hydrochloride (PubChem CID 33611). (GtoPdb)
DESCRIPTION Lofepramine (Lopramine) is a modified tricyclic and orally active antidepressant. Lofepramine inhibits the uptake of Noradrenaline (NA) (HY-13715) and 5-hydroxytryptamine (5-HT) with IC50s of 2.7 ¦ÌM and 11 ¦ÌM, respectively. Lofepramine exerts its antidepressant activity by promoting noradrenergic neurotransmission. Lofepramine also enhances serotonergic neurotransmission by inhibiting neuronal uptake of 5-HT and tryptophan pyrrolase. Lofepramine exhibits significant anxiolytic properties. [1][2][3][4].
PRICE 82
DESCRIPTION High affinity sigma2 agonist (Tocris Bioactive Compound Library)
DESCRIPTION 5-HT and noradrenalin re-uptake inhibitor (SNRI) (Tocriscreen Total)
DESCRIPTION Lofepramine is a serotonin and noradrenalin reuptake inhibitor as an antidepressant. (BOC Sciences Bioactive Compounds)
DESCRIPTION Lofepramine (Leo 640) is a potent tricyclic antidepressant that is extensively metabolized to desipramine. It inhibits the serotonin and norepinephrine transporters by inhibiting neurons with Kd values of 70 and 5.4 nM, respectively, with weak antagonism of serotonin, histamine and muscarinic receptors. (TargetMol Bioactive Compound Library)
Compound Sets
19
BOC Sciences Bioactive Compounds
lofepramine-cas-23047-25-8-item-224949
Cayman Chemical Bioactives
20813
ChEMBL Drugs
CHEMBL87708
CHEMBL2106638
Drug Repurposing Hub
DrugBank
DB13411
DrugCentral
1592
DrugCentral Approved Drugs
1592
DrugMatrix
EUbOPEN Chemogenomics Library
EUB0002624
Guide to Pharmacology
7551
Ki Database
Lofepramine
MedChem Express Bioactive Compound Library
HY-12390
NIH Clinical Collections (NCC)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
TargetMol Bioactive Compound Library
T15773
Tocris Bioactive Compound Library
2545
Tocriscreen Total
External IDs
46
Properties
(calculated by RDKit )
Molecular Weight
418.18
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
0
Rotatable Bonds
7
Ring Count
4
Aromatic Ring Count
3
cLogP
5.78
TPSA
23.55
Fraction CSP3
0.27
Chiral centers
0.0
Largest ring
7.0
QED
0.45
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Primary Target
5-HT Transporters
MOA
Inhibitor
norepinephrine reuptake inhibitor, serotonin–norepinephrine reuptake inhibitor (SNRI)
Target
HTR1A, SLC6A2, SLC6A4
5-HT Receptor
Adrenergic Receptor
norepinephrine reuptake
serotonin reuptake
Indication
depression
Pathway
GPCR/G protein
Neuroscience
Neuronal Signaling
Recommended Cell Concentration
None
Source data