scholarly journals A herbicide structure-activity analysis of the antimalarial lead compound MMV007978 against Arabidopsis thaliana

2018 ◽  
Vol 74 (7) ◽  
pp. 1558-1563 ◽  
Author(s):  
Maxime G Corral ◽  
Julie Leroux ◽  
Stefan Tresch ◽  
Trevor Newton ◽  
Keith A Stubbs ◽  
...  
Keyword(s):  
Arabidopsis Thaliana ◽  
Activity Analysis ◽  
Lead Compound ◽  
Structure Activity

Naldemedine: Peripherally Acting Opioid Receptor Antagonist for Treating Opioid-induced Adverse Effects

2020 ◽  
Vol 20 (31) ◽  
pp. 2830-2842
Author(s):  
Masanao Inagaki ◽  
Toshiyuki Kanemasa ◽  
Takaaki Yokota
Keyword(s):  
Adverse Effects ◽  
Adverse Events ◽  
Severe Pain ◽  
Lead Compound ◽  
Inhibitory Effects ◽  
Pharmacokinetic Profiles ◽  
Structure Activity ◽  
The Usa ◽  
Relationship Study ◽  
The Eu

Opioids are widely used for pain management in moderate-to-severe pain. However, opioids are associated with adverse events, such as constipation and emesis/vomiting. To reduce these undesired effects, a structure–activity relationship study of morphinan derivatives was conducted, and a promising lead compound with inhibitory effects on opioid receptors was obtained. Further improvement in the potency and pharmacokinetic profiles of the lead compound led to the discovery of naldemedine, which showed anti-constipation and anti-emetic effects against these adverse events that were induced by morphine without influencing morphine’s analgesic effect. Naldemedine was launched in Japan and the USA in 2017 and in the EU in 2019, for treating opioid-induced constipation.

A Structure–Activity Analysis of Biased Agonism at the Dopamine D2 Receptor

2013 ◽  
Vol 56 (22) ◽  
pp. 9199-9221 ◽  
Author(s):  
Jeremy Shonberg ◽  
Carmen Klein Herenbrink ◽  
Laura López ◽  
Arthur Christopoulos ◽  
Peter J. Scammells ◽  
...  
Keyword(s):  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Activity Analysis ◽  
Biased Agonism ◽  
Dopamine D2 ◽  
Structure Activity

scholarly journals Clinanthus microstephium , an Amaryllidaceae Species with Cholinesterase Inhibitor Alkaloids: Structure−Activity Analysis of Haemanthamine Skeleton Derivatives

2019 ◽  
Vol 16 (5) ◽  
pp. e1800662
Author(s):  
Tonino G. Adessi ◽  
José L. Borioni ◽  
Natalia B. Pigni ◽  
Jaume Bastida ◽  
Valeria Cavallaro ◽  
...  
Keyword(s):  
Cholinesterase Inhibitor ◽  
Activity Analysis ◽  
Structure Activity

Quantitative Structure−Activity Analysis of the Algae Toxicity of Nitroaromatic Compounds

2000 ◽  
Vol 13 (6) ◽  
pp. 441-450 ◽  
Author(s):  
Heike Schmitt ◽  
Rolf Altenburger ◽  
Bernd Jastorff ◽  
Gerrit Schüürmann
Keyword(s):  
Activity Analysis ◽  
Nitroaromatic Compounds ◽  
Quantitative Structure ◽  
Structure Activity
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