Explore a selection of our essential drug information below, or:
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
Structure for NGX267 (DB05152)
- 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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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.
Target Actions Organism AMuscarinic acetylcholine receptor M1 agonistHumans - 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with NGX267. Ambenonium The risk or severity of adverse effects can be increased when Ambenonium is combined with NGX267. Amikacin The therapeutic efficacy of NGX267 can be decreased when used in combination with Amikacin. Aprotinin The risk or severity of adverse effects can be increased when Aprotinin is combined with NGX267. Atenolol The risk or severity of adverse effects can be increased when Atenolol is combined with NGX267. - 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
- External Links
- PubChem Substance
- 347909984
- ChemSpider
- 8189078
- ZINC
- ZINC000013816318
Clinical Trials
- Clinical Trials
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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
Property Value Source Water Solubility 13.5 mg/mL ALOGPS logP 1.21 ALOGPS logP 1.36 Chemaxon logS -1.2 ALOGPS pKa (Strongest Acidic) 11.85 Chemaxon pKa (Strongest Basic) 8.35 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 32.34 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 58.84 m3·mol-1 Chemaxon Polarizability 23.65 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0090000000-9723efe9f25ccaf64880 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-0090000000-a2077c1b58a72646dcbc Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-01ox-9830000000-686afdc24b43ef3a0997 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-00kb-4940000000-a99fba0c08ac01439049 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0005-9400000000-36908f464913dc8a1bdb Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-052f-4900000000-3d28dc92bbd57a2e040f Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 153.5512958 predictedDarkChem Lite v0.1.0 [M+H]+ 154.1388958 predictedDarkChem Lite v0.1.0 [M+Na]+ 153.9242958 predictedDarkChem Lite v0.1.0
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
- Specific Function
- G protein-coupled acetylcholine receptor activity
- Gene Name
- CHRM1
- Uniprot ID
- P11229
- Uniprot Name
- Muscarinic acetylcholine receptor M1
- Molecular Weight
- 51420.375 Da
References
- 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 October 21, 2007 22:23 / Updated at August 26, 2024 19:23