Identification

Name
NGX267
Accession Number
DB05152
Type
Small Molecule
Groups
Investigational
Description

NGX267 is a muscarinic agonist. It is developed for the treatment of Alzheimer’s disease and has shown the potential to both reduce symptoms and slow disease progression.

Structure
Thumb
Synonyms
Not Available
External IDs
AF-267B / AF267B / NGX-267 / NGX267
Categories
UNII
8D3PZX7G73
CAS number
503431-81-0
Weight
Average: 214.33
Monoisotopic: 214.113984382
Chemical Formula
C10H18N2OS
InChI Key
PHOZOHFUXHPOCK-QMMMGPOBSA-N
InChI
InChI=1S/C10H18N2OS/c1-3-8-9(13)11-10(14-8)4-6-12(2)7-5-10/h8H,3-7H2,1-2H3,(H,11,13)/t8-/m0/s1
IUPAC Name
(2S)-2-ethyl-8-methyl-1-thia-4,8-diazaspiro[4.5]decan-3-one
SMILES
CC[C@@H]1SC2(CCN(C)CC2)NC1=O

Pharmacology

Indication

Investigated for use/treatment in alzheimer's disease and schizophrenia and schizoaffective disorders.

Pharmacodynamics

Due to its mechanism of action, NGX267 may be simultaneously effective in treating the memory and cognitive disturbances experienced by Alzheimer's patients and in reducing the creation of neurotoxic proteins, thereby delaying disease progression.

Mechanism of action

NGX267 has been shown to stimulate M1 receptors in a fashion analogous to acetylcholine, a neurotransmitter essential for memory and cognitive function that is depleted when neurons, or brain cells, degenerate. The M1 receptor plays an important role in memory and cognitive processing. Its activation has also been linked to decreases in two biochemical processes, AB production and tau protein phosphorylation, both of which are involved in the creation of the neurofibrillary tangles and amyloidplaques that are major histopathological hallmarks of Alzheimer's disease. By selectively enhancing M1 cholinergic neurotransmission in the brain, NGX267 may offer advantages over current therapies for Alzheimer's disease due to the relative preservation of this system in patients who are clinically symptomatic.

TargetActionsOrganism
UMuscarinic acetylcholine receptor M1Not 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
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.
DrugInteraction
1,10-PhenanthrolineThe risk or severity of adverse effects can be increased when 1,10-Phenanthroline is combined with NGX267.
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with NGX267.
AcotiamideThe risk or severity of adverse effects can be increased when Acotiamide is combined with NGX267.
AlprenololThe risk or severity of adverse effects can be increased when Alprenolol is combined with NGX267.
AmbenoniumThe risk or severity of adverse effects can be increased when Ambenonium is combined with NGX267.
AmikacinThe therapeutic efficacy of NGX267 can be decreased when used in combination with Amikacin.
AnisodamineThe risk or severity of adverse effects can be increased when Anisodamine is combined with NGX267.
ApramycinThe therapeutic efficacy of NGX267 can be decreased when used in combination with Apramycin.
AprotininThe risk or severity of adverse effects can be increased when Aprotinin is combined with NGX267.
ArbekacinThe therapeutic efficacy of NGX267 can be decreased when used in combination with Arbekacin.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Substance
347909984
ChemSpider
8189078
ZINC
ZINC000013816318

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentDry Mouth / Sjögren's Syndrome1

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 Solubility13.5 mg/mLALOGPS
logP1.21ALOGPS
logP1.36ChemAxon
logS-1.2ALOGPS
pKa (Strongest Acidic)11.85ChemAxon
pKa (Strongest Basic)8.35ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area32.34 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity58.84 m3·mol-1ChemAxon
Polarizability23.65 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
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
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da

Drug created on October 21, 2007 16:23 / Updated on March 01, 2020 19:31

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