Edonerpic

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

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Name
Edonerpic
Accession Number
DB05938
Type
Small Molecule
Groups
Investigational
Description

Edonerpic is a neurotrophic agent intended for the treatment of Alzheimer's disease which is under phase I clinical trial.

Structure
Thumb
Synonyms
Not Available
External IDs
J2.972.359A / T-817
Product Ingredients
IngredientUNIICASInChI Key
Edonerpic maleate0LB9F7I5P3519187-97-4RLUCYBFCLXANSO-BTJKTKAUSA-N
Categories
UNII
QY49O94S2W
CAS number
519187-23-6
Weight
Average: 291.41
Monoisotopic: 291.129300094
Chemical Formula
C16H21NO2S
InChI Key
HQNACSFBDBYLJP-UHFFFAOYSA-N
InChI
InChI=1S/C16H21NO2S/c18-15-11-17(12-15)6-1-7-19-8-4-13-2-3-16-14(10-13)5-9-20-16/h2-3,5,9-10,15,18H,1,4,6-8,11-12H2
IUPAC Name
1-{3-[2-(1-benzothiophen-5-yl)ethoxy]propyl}azetidin-3-ol
SMILES
OC1CN(CCCOCCC2=CC3=C(SC=C3)C=C2)C1

Pharmacology

Indication

Investigated for use/treatment in alzheimer's disease.

Pharmacodynamics
Not Available
Mechanism of action

T-817MA has neuroprotective properties. Toyama Chemical has demonstrated that T-817MA prevents neurodegeneration induced by Amyloid-b protein. Accumulation of Amyloid-b protein is considered to be central to the pathogenesis of Alzheimer's disease. The neuroprotective properties of T-817MA were also observed in a mutant tau induced Alzheimer's disease model. Besides these neuroprotective properties, T-817MA also promotes neurite outgrowth.

TargetActionsOrganism
UAmyloid beta A4 proteinNot AvailableHumans
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
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
  1. Hirata K, Yamaguchi H, Takamura Y, Takagi A, Fukushima T, Iwakami N, Saitoh A, Nakagawa M, Yamada T: A novel neurotrophic agent, T-817MA [1-{3-[2-(1-benzothiophen-5-yl) ethoxy] propyl}-3-azetidinol maleate], attenuates amyloid-beta-induced neurotoxicity and promotes neurite outgrowth in rat cultured central nervous system neurons. J Pharmacol Exp Ther. 2005 Jul;314(1):252-9. Epub 2005 Mar 29. [PubMed:15798005]
  2. Yamashita D, Shiotani A, Kanzaki S, Nakagawa M, Ogawa K: Neuroprotective effects of T-817MA against noise-induced hearing loss. Neurosci Res. 2008 May;61(1):38-42. doi: 10.1016/j.neures.2008.01.009. Epub 2008 Jan 29. [PubMed:18343519]
  3. Seo T, Sumiyoshi T, Tsunoda M, Tanaka K, Uehara T, Matsuoka T, Itoh H, Kurachi M: T-817MA, a novel neurotrophic compound, ameliorates phencyclidine-induced disruption of sensorimotor gating. Psychopharmacology (Berl). 2008 Apr;197(3):457-64. doi: 10.1007/s00213-007-1057-8. Epub 2008 Feb 5. [PubMed:18251012]
External Links
ChemSpider
8077600

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceHealthy Volunteers / Hepatic Impairment1
2CompletedTreatmentAlzheimer's Disease (AD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0404 mg/mLALOGPS
logP2.82ALOGPS
logP2.29ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)14.79ChemAxon
pKa (Strongest Basic)7.24ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area32.7 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity82.6 m3·mol-1ChemAxon
Polarizability33.5 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transition metal ion binding
Specific Function
Functions as a cell surface receptor and performs physiological functions on the surface of neurons relevant to neurite growth, neuronal adhesion and axonogenesis. Involved in cell mobility and tra...
Gene Name
APP
Uniprot ID
P05067
Uniprot Name
Amyloid beta A4 protein
Molecular Weight
86942.715 Da

Drug created on November 18, 2007 11:28 / Updated on June 04, 2019 06:20