英文名称 | AQW051 |
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别名 | AQW-051;VQW 765;VQW-765;VQW765 |
英文别名 | AQW-051;VQW 765;VQW-765;VQW765 |
IUPAC Name | (3R)-3-[6-(4-methylphenyl)pyridin-3-yl]oxy-1-azabicyclo[2.2.2]octane |
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INCHI | InChI=1S/C19H22N2O/c1-14-2-4-15(5-3-14)18-7-6-17(12-20-18)22-19-13-21-10-8-16(19)9-11-21/h2-7,12,16,19H,8-11,13H2,1H3/t19-/m0/s1 |
InChi Key | NPDLTEZXGWRMLQ-IBGZPJMESA-N |
Canonical SMILES | CC1=CC=C(C=C1)C2=NC=C(C=C2)OC3CN4CCC3CC4 |
关联CAS | 669770-29-0 |
PubChem CID | 50914822 |
MeSH Entry Terms | 3-(6-p-tolylpyridin-3-yloxy)-1-azabicyclo(2.2.2)octane;AQW051 |
PubChem CID | 50914822 |
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CAS Registry No. | 669770-29-0 |
ChEMBL Ligand | CHEMBL4532388 |
BindingDB Ligand | 50520725 |
Ligand ID | 7371 |
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名称 | AQW051 |
别名 | AQW-051 |
类别 | Synthetic organic |
学名 | (3R)-3-{[6-(4-methylphenyl)pyridin-3-yl]oxy}-1-azabicyclo[2.2.2]octane |
生物活性评价 |
AQW051 demonstrates high affinity for nAChR α7 as a potent agonist |
评价 |
AQW 051 is an α7 nicotinic acetylcholine receptor (nAChR) partial agonist from Novartis for the oral treatment of cognitive deficits in schizophrenia, Alzheimer's, and Parkinson's diseases |
临床描述 |
This is a multicenter, randomized, double-blind, placebo-controlled study to evaluate the
efficacy and safety of a single oral dose of VQW-765 compared to placebo in male and female
participants with performance anxiety.
This study will assess the safety, tolerability and efficacy of AQW051 in treating moderate to severe L-dopa induced dyskinesias (movement disorders) in patients with Parkinson's disease. |
来源公司 |
Vanda Pharmaceuticals Novartis |
1. Di Paolo T, Grégoire L, Feuerbach D, Elbast W, Weiss M, Gomez-Mancilla B. (2014) AQW051, a novel and selective nicotinic acetylcholine receptor α7 partial agonist, reduces l-Dopa-induced dyskinesias and extends the duration of l-Dopa effects in parkinsonian monkeys.. Parkinsonism Relat Disord, 20 (11): (1119-23). [PMID:25172125] |
2. Feuerbach D, Pezous N, Weiss M, Shakeri-Nejad K, Lingenhoehl K, Hoyer D, Hurth K, Bilbe G, Pryce CR, McAllister K et al.. (2015) AQW051, a novel, potent and selective α7 nicotinic ACh receptor partial agonist: pharmacological characterization and phase I evaluation.. Br J Pharmacol, 172 (5): (1292-304). [PMID:25363835] |