Traxoprodil

Identification

Generic Name
Traxoprodil
DrugBank Accession Number
DB18795
Background

Not Available

Type
Small Molecule
Groups
Investigational
Structure
Weight
Average: 327.424
Monoisotopic: 327.183443669
Chemical Formula
C20H25NO3
Synonyms
  • (.alpha.s,.beta.s)-4-hydroxy-.alpha.-(p-hydroxyphenyl)-.beta.-methyl-4-phenyl-1-piperidineethanol
  • 1-piperidineethanol, 4-hydroxy-.alpha.-(4-hydroxyphenyl)-.beta.-methyl-4-phenyl-, (s-(r*,r*))-
External IDs
  • CP-101,606
  • CP-101606

Pharmacology

Indication

Not Available

Reduce drug development failure rates
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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action
TargetActionsOrganism
AGlutamate receptor ionotropic, NMDA 2B
antagonist
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Not Available
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
UTC046R5HM
CAS number
134234-12-1
InChI Key
QEMSVZNTSXPFJA-HNAYVOBHSA-N
InChI
InChI=1S/C20H25NO3/c1-15(19(23)16-7-9-18(22)10-8-16)21-13-11-20(24,12-14-21)17-5-3-2-4-6-17/h2-10,15,19,22-24H,11-14H2,1H3/t15-,19+/m0/s1
IUPAC Name
SMILES
C[C@@H]([C@@H](O)C1=CC=C(O)C=C1)N1CCC(O)(CC1)C1=CC=CC=C1

References

General References
Not Available
ChemSpider
189919
BindingDB
50032651
ChEMBL
CHEMBL17350
ZINC
ZINC000000005936
Wikipedia
Traxoprodil

Clinical Trials

Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
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PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
2CompletedTreatmentMajor Depressive Disorder (MDD)1somestatusstop reasonjust information to hide
2CompletedTreatmentParkinson's Disease (PD)1somestatusstop reasonjust information to hide
2TerminatedTreatmentStroke1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Component of NMDA receptor complexes that function as heterotetrameric, ligand-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Channel activation requires binding of the neurotransmitter glutamate to the epsilon subunit, glycine binding to the zeta subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+) (PubMed:26875626, PubMed:26919761, PubMed:28126851, PubMed:8768735). Sensitivity to glutamate and channel kinetics depend on the subunit composition (PubMed:26875626, PubMed:8768735). In concert with DAPK1 at extrasynaptic sites, acts as a central mediator for stroke damage. Its phosphorylation at Ser-1303 by DAPK1 enhances synaptic NMDA receptor channel activity inducing injurious Ca2+ influx through them, resulting in an irreversible neuronal death. Contributes to neural pattern formation in the developing brain. Plays a role in long-term depression (LTD) of hippocampus membrane currents and in synaptic plasticity (By similarity).
Specific Function
amyloid-beta binding
Gene Name
GRIN2B
Uniprot ID
Q13224
Uniprot Name
Glutamate receptor ionotropic, NMDA 2B
Molecular Weight
166365.885 Da
References
  1. Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]

Drug created at June 21, 2024 16:53 / Updated at August 27, 2024 19:17