scholarly journals Selective κ receptor partial agonist HS666 produces potent antinociception without inducing aversion after i.c.v. administration in mice

2017 ◽  
Vol 174 (15) ◽  
pp. 2444-2456 ◽  
Author(s):  
Mariana Spetea ◽  
Shainnel O Eans ◽  
Michelle L Ganno ◽  
Aquilino Lantero ◽  
Michael Mairegger ◽  
...  
Keyword(s):  
Partial Agonist ◽  
Κ Receptor

Tegaserod, a 5HT4 receptor partial agonist, devoid of significant electrocardiographic effects

2001 ◽  
Vol 120 (5) ◽  
pp. A643-A643
Author(s):  
P RUEEGG ◽  
C BALDAUF ◽  
S DINGEMANSE ◽  
M LEFKOWITZ ◽  
J MORGANROTH
Keyword(s):  
Partial Agonist

Washington Agonizes Over a Partial-Agonist

2004 ◽  
Author(s):  
Geoff Mumford
Keyword(s):  
Partial Agonist

Methoclocinnamox: A Mu Partial Agonist With Pharmacotherapeutic Potential for Heroin Abuse

1995 ◽  
Author(s):  
James H. Woods ◽  
◽  
John W. Lewis ◽  
Gail Winger ◽  
Eduardo Butelman ◽  
...  
Keyword(s):  
Partial Agonist ◽  
Heroin Abuse

Cytisine as an alternative smoking cessation product for Pacific smokers in New Zealand

2018 ◽  
Vol 21 (2) ◽  
pp. 89-95
Author(s):  
Vili Nosa ◽  
Kotalo Leau ◽  
Natalie Walker
Keyword(s):  
Smoking Cessation ◽  
New Zealand ◽  
Nicotinic Acetylcholine Receptors ◽  
Cultural Practices ◽  
Partial Agonist ◽  
Snowball Sampling ◽  
Structured Interviews ◽  
Liquid Form ◽  
Pacific People ◽  
The Pacific

ABSTRACT Introduction: Pacific people in New Zealand have one of the highest rates of smoking.  Cytisine is a plant-based alkaloid that has proven efficacy, effectiveness and safety compared to a placebo and nicotine replacement therapy (NRT) for smoking cessation.  Cytisine, like varenicline, is a partial agonist of nicotinic acetylcholine receptors, and blocks the rewarding effects of nicotine. Cytisine is naturally found in some plants in the Pacific region, and so may appeal to Pacific smokers wanting to quit. This paper investigates the acceptability of cytisine as a smoking cessation product for Pacific smokers in New Zealand, using a qualitative study design. Methods: In December 2015, advertisements and snowball sampling was used to recruit four Pacific smokers and three Pacific smoking cessation specialists in Auckland, New Zealand. Semi-structured interviews where undertaken, whereby participants were asked about motivations to quit and their views on smoking cessation products, including cytisine (which is currently unavailable in New Zealand). Interviews were recorded and transcribed verbatim, with thematic analysis conducted manually. Findings: Pacific smokers reported wanting to quit for loved ones and family, but did not find currently available smoking cessation products effective. Almost all participants had not previously heard of cytisine, but many of the Pacific smokers were keen to try it. Participants identified with cytisine on a cultural basis (given its natural status), but noted that their use would be determined by the efficacy of the medicine, its cost, side-effects, and accessibility. They were particularly interested in cytisine being made available in liquid form, which could be added to a “smoothie” or drunk as a “traditional tea”.  Participants thought cytisine should be promoted in a culturally-appropriate way, with packaging and advertising designed to appeal to Pacific smokers. Conclusions: Cytisine is more acceptable to Pacific smokers than other smoking cessation products, because of their cultural practices of traditional medicine and the natural product status of cytisine.

In silico Discovery of Resveratrol Analogues as Potential Agents in Treatment of Metabolic Disorders

2019 ◽  
Vol 25 (35) ◽  
pp. 3776-3783
Author(s):  
Nebojša Pavlović ◽  
Maja Đanić ◽  
Bojan Stanimirov ◽  
Svetlana Goločorbin-Kon ◽  
Karmen Stankov ◽  
...  
Keyword(s):  
In Silico ◽  
Metabolic Disorders ◽  
Partial Agonist ◽  
Aqueous Solubility ◽  
Structural Similarity ◽  
Data Bank ◽  
Docking Studies ◽  
Binding Energies ◽  
Molegro Virtual Docker ◽  
Ppar Γ

Background: Resveratrol was demonstrated to act as partial agonist of PPAR-γ receptor, which opens up the possibility for its use in the treatment of metabolic disorders. Considering the poor bioavailability of resveratrol, particularly due to its low aqueous solubility, we aimed to identify analogues of resveratrol with improved pharmacokinetic properties and higher binding affinities towards PPAR-γ. Methods: 3D structures of resveratrol and its analogues were retrieved from ZINC database, while PPAR-γ structure was obtained from Protein Data Bank. Docking studies were performed using Molegro Virtual Docker software. Molecular descriptors relevant to pharmacokinetics were calculated from ligand structures using VolSurf+ software. Results: Using structural similarity search method, 56 analogues of resveratrol were identified and subjected to docking analyses. Binding energies were ranged from -136.69 to -90.89 kcal/mol, with 16 analogues having higher affinities towards PPAR-γ in comparison to resveratrol. From the calculated values of SOLY descriptor, 23 studied compounds were shown to be more soluble in water than resveratrol. However, only two tetrahydroxy stilbene derivatives, piceatannol and oxyresveratrol, had both better solubility and affinity towards PPAR-γ. These compounds also had more favorable ADME profile, since they were shown to be more metabolically stable and wider distributed in body than resveratrol. Conclusion: Piceatannol and oxyresveratrol should be considered as potential lead compounds for further drug development. Although experimental validation of obtained in silico results is required, this work can be considered as a step toward the discovery of new natural and safe drugs in treatment of metabolic disorders.

Does the Oxazolidinone Derivatives Constitute a Functional Approach for Cancer Therapy?

2020 ◽  
Vol 7 (2) ◽  
pp. 95-106
Author(s):  
Eduardo Augusto Vasconcelos de Freitas Ramalho ◽  
Marina Galdino da Rocha Pitta ◽  
Hernando de Barros Siqueira Neto ◽  
Ivan da Rocha Pitta
Keyword(s):  
Cell Lines ◽  
Antitumor Agents ◽  
Partial Agonist ◽  
Drug Repurposing ◽  
Antitumor Agent ◽  
Short Review ◽  
Sphingolipid Metabolism ◽  
Solid Cancer ◽  
Ppar Γ ◽  
Anti Cancer

In the last four decades, the emphasis was laid on the research of small organic molecules with potential anti-cancer activity. Linezolid was the first oxazolidinone derivative approved by FDA for MRSA treatment. Despite its major role in antimicrobial activity, these molecules display other properties, also serving as an antitumor agent. The importance of drug repurposing could be highlighted by the use of Oxazolidinone derivatives in pre-clinical studies, which are able to act through different pathways, such as partial agonist of transcription factor PPAR-γ, an inhibitor of key enzymes related to hormone-dependent disorders and even on sphingolipid metabolism as well. The purpose of this short review is to discuss the application of oxazolidinone derivatives as an antitumor agent by highlighting the most promising molecules studied by many research groups worldwide. Main biological activity against several tumor cell lines, including hematopoietic and solid cancer cell lines have been discussed. In addition, this study intends to report how different types of oxazolidinone derivatives can act as antitumor agents describing their distinct mechanisms of action based on their targets.

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