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
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
DescriptionCurator'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
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
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL216 |
30.0 nM [EC50] | ||
Target ID: CHEMBL211 |
1.57 µM [EC50] | ||
Target ID: CHEMBL1821 |
1.56 µM [EC50] | ||
Target ID: CHEMBL245 |
44.0 nM [EC50] | ||
Target ID: CHEMBL2035 |
0.85 µM [EC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| ["Sleep attacks" in Parkinson patients. A side effect of nonergoline dopamine agonists or a class effect of dopamine agonists?]. | 2000 Aug |
|
| High-dose therapy with ropinirole in patients with Parkinson's disease. | 2001 |
|
| Increased risk of somnolence with the new dopamine agonists in patients with Parkinson's disease: a meta-analysis of randomised controlled trials. | 2001 |
|
| Sleep disorders in patients with Parkinson's disease: epidemiology and management. | 2001 |
|
| Are dopamine receptor agonists neuroprotective in Parkinson's disease? | 2001 |
|
| Neostriatal muscarinic receptor subtypes involved in the generation of tremulous jaw movements in rodents implications for cholinergic involvement in parkinsonism. | 2001 Apr 27 |
|
| Iontophoretic delivery of ropinirole hydrochloride: effect of current density and vehicle formulation. | 2001 Dec |
|
| [Dopamine agonists situation in Parkinson disease]. | 2001 Dec 1-15 |
|
| Efficacy and tolerability of dopamine agonists in a parkinsonian population. | 2001 Feb |
|
| Molecular mechanism in activation of glutathione system by ropinirole, a selective dopamine D2 agonist. | 2001 Jan |
|
| Adjunctive dopamine agonists in treatment-resistant bipolar II depression: an open case series. | 2001 Jul |
|
| Antiparkinsonian activity and dyskinesia risk of ropinirole and L-DOPA combination therapy in drug naïve MPTP-lesioned common marmosets (Callithrix jacchus). | 2001 Jul |
|
| The frissonnant mutant mouse, a model of dopamino-sensitive, inherited motor syndrome. | 2001 Jun |
|
| [Parkinson disease: diagnostic and therapeutic criteria]. | 2001 Mar 3 |
|
| Sleep attacks and antiparkinsonian drugs: a pilot prospective pharmacoepidemiologic study. | 2001 May-Jun |
|
| Warfarin and ropinirole interaction. | 2001 Oct |
|
| Daytime sleepiness and other sleep disorders in Parkinson's disease. | 2001 Oct 23 |
|
| Randomized clinical trials with added rescue medication: some approaches to their analysis and interpretation. | 2001 Oct 30 |
|
| 'Sleep attacks' or 'unintended sleep episodes' occur with dopamine agonists: is this a class effect? | 2002 |
|
| Clinical pharmacokinetic and pharmacodynamic properties of drugs used in the treatment of Parkinson's disease. | 2002 |
|
| Excessive daytime sleepiness and sudden-onset sleep in Parkinson disease: a survey by the Canadian Movement Disorders Group. | 2002 Jan 23-30 |
|
| Pergolide in the treatment of patients with early and advanced Parkinson's disease. | 2002 Jan-Feb |
|
| Gateways to clinical trials. | 2002 Jul-Aug |
|
| Effect of dopamine receptor agonists on sensory nerve activity: possible therapeutic targets for the treatment of asthma and COPD. | 2002 Jun |
|
| Behavioral and neurochemical effects of dopaminergic drugs in models of brain injury. | 2002 Jun |
|
| Sleep attacks in patients taking dopamine agonists: review. | 2002 Jun 22 |
|
| Gateways to clinical trials. | 2002 May |
|
| Ropinirole for the treatment of tremor in early Parkinson's disease. | 2002 May |
|
| Levodopa but not ropinirole induces an internalization of D1 dopamine receptors in parkinsonian rats. | 2002 Nov |
|
| Do dopamine agonists or levodopa modify Parkinson's disease progression? | 2002 Nov |
|
| Dopamine agonists and neuroprotection in Parkinson's disease. | 2002 Nov |
|
| Practical importance of neuroprotection in Parkinson's disease. | 2002 Oct |
|
| Neuroprotection in idiopathic Parkinson's disease. | 2002 Oct |
|
| 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 Sep |
|
| Ropinirole in restless leg syndrome. | 2002 Sep-Oct |
|
| Cabergoline, pramipexole and ropinirole used as monotherapy in early Parkinson's disease: an evidence-based comparison. | 2003 |
|
| Sleep attacks--facts and fiction: a critical review. | 2003 |
|
| Current status of Parkinson's disease treatment in Korea. | 2003 Aug |
|
| Parkinson's disease: is the initial treatment established? | 2003 Jul |
|
| Dual dopamine agonist treatment in Parkinson's disease. | 2003 Jul |
|
| Slower progression of Parkinson's disease with ropinirole versus levodopa: The REAL-PET study. | 2003 Jul |
|
| Sleep attacks, daytime sleepiness, and dopamine agonists in Parkinson's disease. | 2003 Jun |
|
| Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole. | 2003 Nov |
|
| Clinical strategies to prevent and delay motor complications. | 2003 Sep 23 |
Patents
Sample Use Guides
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Code | English |
| Code System | Code | Type | Description | ||
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DB05152
Created by
admin on Sat Dec 16 02:31:12 GMT 2023 , Edited by admin on Sat Dec 16 02:31:12 GMT 2023
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503431-81-0
Created by
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10013505
Created by
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DTXSID40198399
Created by
admin on Sat Dec 16 02:31:12 GMT 2023 , Edited by admin on Sat Dec 16 02:31:12 GMT 2023
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8D3PZX7G73
Created by
admin on Sat Dec 16 02:31:12 GMT 2023 , Edited by admin on Sat Dec 16 02:31:12 GMT 2023
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SUBSTANCE RECORD
