NGX-267

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C10H18N2OS
Molecular Weight	214.328
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC[C@@H]1SC2(CCN(C)CC2)NC1=O

InChI

InChIKey=PHOZOHFUXHPOCK-QMMMGPOBSA-N

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

HIDE SMILES / InChI

Molecular Formula	C10H18N2OS
Molecular Weight	214.328
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19168056
Curator's Comment: The description was created based on several sources, including https://www.drugbank.ca/drugs/DB05152 | https://clinicaltrials.gov/ct2/show/NCT00637793 | https://www.ncbi.nlm.nih.gov/pubmed/12212772 | https://www.ncbi.nlm.nih.gov/pubmed/19212877 | https://www.ncbi.nlm.nih.gov/pubmed/18220527

NGX267 is a partial muscarinic receptor agonist with functionally specific M1 and M3 receptor activity, developed by Torrey Pines Therapeutics(TPTX) for the treatment of Xerostomia, Alzheimer’s disease and cognitive deficits in schizophrenia. NGX-267 had been in phase II clinical trials for the treatment of Xerostomia, however, all researchers on this drug candidate were discontinued.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Muscarinic acetylcholine receptor M1 168 Target ID: CHEMBL216 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19168056	Agonist 2752	30.0 nM [EC50]
Muscarinic acetylcholine receptor M2 121 Target ID: CHEMBL211 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19168056	Agonist 2752	1.57 µM [EC50]
Muscarinic acetylcholine receptor M4 87 Target ID: CHEMBL1821 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19168056	Agonist 2752	1.56 µM [EC50]
Muscarinic acetylcholine receptor M3 160 Target ID: CHEMBL245 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19168056	Agonist 2752	44.0 nM [EC50]
Muscarinic acetylcholine receptor M5 63 Target ID: CHEMBL2035 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19168056	Partial Agonist 297	0.85 µM [EC50]

Conditions

Condition	Modality	Highest Phase	Product
Xerostomia 1 Sources: https://clinicaltrials.gov/ct2/show/NCT00637793	Primary	Phase II 1147	Unknown Approved Use Unknown
Sjogren's syndrome 8 Sources: https://clinicaltrials.gov/ct2/show/NCT00637793	Primary	Phase II 1147	Unknown Approved Use Unknown
Alzheimer’s disease 278 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14501019	Primary	Phase I 438	Unknown Approved Use Unknown

Sourcing

Vendor/Aggregator	ID	URL
1PlusChem LLC	1P00DFUD	https://www.1pchem.com/search?query=1P00DFUD
Angene	AGN-PC-0OBBE4	http://www.angenechemical.com/productshow/AGN-PC-0OBBE4.html
AOBIOUS INC	AOB5052	http://aobious.com/aobious/search?search_query=AOB5052
AstaTech	C90302	http://astatechinc.com/CPSResult.php?CRNO=C90302
BOC Sciences	503431-81-0	http://www.bocsci.com/description.asp?cas=503431-81-0
Chemspace	CSC010467217	https://chem-space.com/CSC010467217
Chemspace	CSC015360454	https://chem-space.com/CSC015360454
eMolecules	27519972	https://orderbb.emolecules.com/search/#?query=27519972
Enamine	BBV-45273137	http://www.enaminestore.com/catalog/BBV-45273137
Enamine	BBV-79325237	http://www.enaminestore.com/catalog/BBV-79325237
mcule	MCULE-1468174777	https://mcule.com/MCULE-1468174777/
MolPort	MolPort-003-847-292	https://www.molport.com/shop/molecule-link/MolPort-003-847-292
MuseChem	R007567	https://www.musechem.com/product/R007567.html
PepTech	MFCD09265248	http://www.peptechcorp.com/products/productSearch.asp?searchString=MFCD09265248
PepTech	RC780-1	http://www.peptechcorp.com/products/productSearch.asp?searchString=RC780-1
Toronto Research Chemicals	E925120	https://www.trc-canada.com/product-detail/?CatNum=E925120
Toronto Research Chemicals	M328280	https://www.trc-canada.com/product-detail/?CatNum=M328280
Wonderchem	WD068IJ	http://www.wonder-chem.com/search.html?text=WD068IJ

PubMed

Title	Date	PubMed
Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole.	2003-11	14535946
Dopamine receptor agonists in current clinical use: comparative dopamine receptor binding profiles defined in the human striatum.	2003-10	14523624
Current treatment options for restless legs syndrome.	2003-10	14521483
Clinical strategies to prevent and delay motor complications.	2003-09-23	14504375
Current status of Parkinson's disease treatment in Korea.	2003-08	12915074
Parkinson's disease: is the initial treatment established?	2003-07	12930698
Dual dopamine agonist treatment in Parkinson's disease.	2003-07	12883924
Slower progression of Parkinson's disease with ropinirole versus levodopa: The REAL-PET study.	2003-07	12838524
REAL and CALM: what have we learned?	2003-07	12815670
High-dose ropinirole in advanced Parkinson's disease with severe dyskinesias.	2003-06-05	12782917
Sleep attacks, daytime sleepiness, and dopamine agonists in Parkinson's disease.	2003-06	12784269
The increased utilisation of dopamine agonists and the introduction of COMT inhibitors have not reduced levodopa consumption--a nation-wide perspective in Sweden.	2003-06	12781593
[Pseudopheochromocytoma in Parkinson disease and depression].	2003-05	14509040
The initial drug treatment of older patients with Parkinson's disease - consider an agonist, but don't demonise dopa.	2003-05	12720606
Dihydroergocriptine in Parkinson's disease: clinical efficacy and comparison with other dopamine agonists.	2003-05	12713527
[Sexual delinquency and Parkinson's disease].	2003-04	12707708
Slowing Parkinson's disease progression: recent dopamine agonist trials.	2003-02-11	12580184
Piribedil-induced sleep attacks in Parkinson's disease.	2003-02	12588638
Ropinirole as an adjunct to levodopa in the treatment of Parkinson's disease A short commentary.	2003-01	12528000
Ropinirole as an adjunct to levodopa in the treatment of Parkinson's disease: a 16-week bromocriptine controlled study.	2003-01	12527999
Gabapentin versus ropinirole in the treatment of idiopathic restless legs syndrome.	2003	14504416
Cabergoline, pramipexole and ropinirole used as monotherapy in early Parkinson's disease: an evidence-based comparison.	2003	12964891
Comparison of the risk of adverse events with pramipexole and ropinirole in patients with Parkinson's disease: a meta-analysis.	2003	12688834
Cost analysis of ropinirole versus levodopa in the treatment of Parkinson's disease.	2003	12515573
The timing of antiparkinsonian treatment reduction after subthalamic nucleus stimulation.	2003	12464720
Dopamine agonists induce episodes of irresistible daytime sleepiness.	2003	12464715
Sleep attacks--facts and fiction: a critical review.	2003	12442691
Ropinirole in restless leg syndrome.	2002-12-05	12462942
A comparison of the progression of early Parkinson's disease in patients started on ropinirole or L-dopa: an 18F-dopa PET study.	2002-12	12486484
Dopamine agonist monotherapy in Parkinson's disease.	2002-11-30	12480442
Levodopa but not ropinirole induces an internalization of D1 dopamine receptors in parkinsonian rats.	2002-11	12465054
Do dopamine agonists or levodopa modify Parkinson's disease progression?	2002-11	12464117
Dopamine agonists and neuroprotection in Parkinson's disease.	2002-11	12464116
Ropinirole for antidepressant-induced sexual dysfunction.	2002-11	12409684
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor.	2002-11	12388667
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.	2002-11	12388666
Practical importance of neuroprotection in Parkinson's disease.	2002-10	12522574
Neuroprotection in idiopathic Parkinson's disease.	2002-10	12522567
An evidence-based review of dopamine receptor agonists in the treatment of Parkinson's disease.	2002-10	12436117
Dosing with ropinirole in a clinical setting.	2002-10	12225314
[The usefulness of dopaminergic drugs in traumatic brain injury].	2002-09-18	12235569
Gateways to clinical trials.	2002-09-13	12224444
Do dopaminergic agents increase the daytime sleep propensity? Article reviewed: Effect of ropinirole on sleep onset. A randomized, placebo-controlled study in healthy volunteers.	2002-09	14592182
Combination of two different dopamine agonists in the management of Parkinson's disease.	2002-09	12548370
Alterations in striatal neuropeptide mRNA produced by repeated administration of L-DOPA, ropinirole or bromocriptine correlate with dyskinesia induction in MPTP-treated common marmosets.	2002	12453478
Restless legs syndrome in the older adult: diagnosis and management.	2002	12390051
Sleep disorders in Parkinson's disease: epidemiology and management.	2002	12390050
[Use of dopamine agonists in the treatment of Parkinson's disease].	2002	12378886
DA agonists -- non-ergot derivatives: ropinirole: management of Parkinson's disease.	2002	12211149
Choosing the right dopamine agonist for patients with Parkinson's disease.	2002	12201621

Patents

Sample Use Guides

In Vivo Use Guide

1 -35 mg as single oral dose

Route of Administration: Oral

In Vitro Use Guide

PC12 cells stably transfected with M1 mAChR were used for activity evaluation. Cells were treated with NGX267(50ng/mL). NGX267 inhibit Abeta- and oxidative-stress-induced cell death and apoptosis in PC12 cells transfected with the M1 muscarinic receptor.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 21:13:47 GMT 2025` Edited by `admin` on `Mon Mar 31 21:13:47 GMT 2025`
Record UNII	8D3PZX7G73
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

AF-267B

Preferred Name

English

NGX-267

Common Name

English

NGX267

Code

English

1-THIA-4,8-DIAZASPIRO(4.5)DECAN-3-ONE, 2-ETHYL-8-METHYL-, (2S)-

Systematic Name

English

Code System Code Type Description

DRUG BANK

DB05152