General
Preferred name
PROTRIPTYLINE
Synonyms
PROTRYPTYLINE HYDROCHLORIDE ()
PROTRIPTYLINE HYDROCHLORIDE ()
Protriptyline HCl ()
Protryptyline ()
Protriptyline (hydrochloride) ()
Concordin-5 ()
Concordin-10 ()
Vivactil ()
MK-240 ()
NSC-169912 ()
P&D ID
PD010089
CAS
1225-55-4
438-60-8
Tags
natural product
drug
available
Approved by
FDA
First approval
1967
Drug Status
approved
Drug indication
Depression
Antidepressant
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS Protriptyline is a tricyclic antidepressant. It was thought that tricyclic antidepressants work by inhibiting the reuptake of the neurotransmitters norepinephrine and serotonin by nerve cells. The effectiveness of antidepressants appear after approximately two weeks following recommended adminsitration schedule. Gradual changes are thought to occur in the cerebral cortex and hippocampus, involved in emotion regulation as part of the limbic system, as receptor sensitivity is enhanced. While α1 and β1 receptors are sensitized, α2 receptors are desensitized (leading to increased noradrenaline production). Tricyclics are also reported to alter the perceptions of pain, including neuropathic or neuralgic pain, so they may exhibit analgesic properties. The mechanism of action behind this analgesic property is not fully understood; however, it is thought to involve modulation of endogenous opioid systems in the CNS via an indirect serotonergic route. Tricyclic antidepressants are also effective in relieving migraine prophylaxis, but not in abortion of acute migraine attack, potentially via their serotonergic effects.
DESCRIPTION Protriptyline is a tricyclic antidepressant.
Marketed formulations may contain protriptyline hydrochloride (PubChem CID 6603149). (GtoPdb)
ROE Protriptyline is reported to undergo cumulative urinary excretion during 16 days, which accounts for approximately 50% of the total drug administered. The fecal excretion pathway seems to play a minimal role in drug elimination.
DESCRIPTION Norepinephrine reuptake blocker (LOPAC library)
Cell lines
1
Organisms
1
Compound Sets
28
Cayman Chemical Bioactives
31179
ChEMBL Approved Drugs
CHEMBL1200332
CHEMBL668
ChEMBL Drugs
CHEMBL1200332
CHEMBL668
Concise Guide to Pharmacology 2017/18
7285
Concise Guide to Pharmacology 2019/20
7285
Concise Guide to Pharmacology 2021/22
7285
Concise Guide to Pharmacology 2023/24
7285
Drug Repurposing Hub
DrugBank
DB00344
DrugBank Approved Drugs
DB00344
DrugCentral
2320
DrugCentral Approved Drugs
2320
DrugMAP
DMNHTZI
DrugMAP Approved Drugs
DMNHTZI
DrugMatrix
EU-OPENSCREEN Bioactive Compound Library
EOS100375
Guide to Pharmacology
7285
Ki Database
Protriptyline
Protryptyline
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL668
MedChem Express Bioactive Compound Library
HY-B0949
NCATS Inxight Approved Drugs
4NDU154T12
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
protriptyline-hydrochloride
TargetMol Bioactive Compound Library
T0204
The Spectrum Collection
External IDs
50
Properties
(calculated by RDKit )
Molecular Weight
263.17
Hydrogen Bond Acceptors
1
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
3
Aromatic Ring Count
2
cLogP
4.3
TPSA
12.03
Fraction CSP3
0.26
Chiral centers
0.0
Largest ring
7.0
QED
0.81
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
Reuptake
Pathway
GPCR/G protein
Neuroscience
Neuronal Signaling
Target
Sert (Sodium-dependent)
SLC6A2, SLC6A4
Cholinesterase (ChE)
5-HT Receptor
Indication
depression
MOA
tricyclic antidepressant
Therapeutic Class
Antidepressants
Source data