Identification

Generic Name
NGX267
DrugBank Accession Number
DB05152
Background

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.

Type
Small Molecule
Groups
Investigational
Structure
Weight
Average: 214.33
Monoisotopic: 214.113984382
Chemical Formula
C10H18N2OS
Synonyms
Not Available
External IDs
  • AF-267B
  • AF267B
  • NGX-267
  • NGX267

Pharmacology

Indication

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

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Contraindications & Blackbox Warnings
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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

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.
DrugInteraction
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol 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.
AprotininThe risk or severity of adverse effects can be increased when Aprotinin is combined with NGX267.
AtenololThe risk or severity of adverse effects can be increased when Atenolol is combined with NGX267.
BetaineThe risk or severity of adverse effects can be increased when Betaine is combined with NGX267.
BetaxololThe risk or severity of adverse effects can be increased when Betaxolol is combined with NGX267.
BisoprololThe risk or severity of adverse effects can be increased when Bisoprolol is combined with NGX267.
CapreomycinThe therapeutic efficacy of NGX267 can be decreased when used in combination with Capreomycin.
CapsaicinThe risk or severity of adverse effects can be increased when Capsaicin is combined with NGX267.
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Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
8D3PZX7G73
CAS number
503431-81-0
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

References

General References
Not Available
PubChem Substance
347909984
ChemSpider
8189078
ZINC
ZINC000013816318

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentDry Mouth / Sjogren's Syndrome (SS)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 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

Targets

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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 at October 21, 2007 22:23 / Updated at June 12, 2020 16:52