Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery
Heterocyclic amino derivatives have been extensively synthesized and validated as potent bioactive compounds, and nowadays, numerous marketed drugs share these scaffolds, from very simple structures (monoamino, monocyclic compounds) to much more complex ...
Tony Ge, Jean-Christophe Cintrat
doaj +1 more source
Interaction of hypothalamic GABA\u3csub\u3eA\u3c/sub\u3e and excitatory amino acid receptors controlling heart rate in rats [PDF]
We have previously shown that microinjection of drugs that impair gamma-aminobutyric acid (GABA)-mediated synaptic inhibition into the dorsomedial hypothalamus (DMH) of rats generates cardiovascular and behavioral changes that mimic the response to ...
DiMicco, Joseph A., Soltis, Robert P.
core +2 more sources
ACSEE: Antagonistic Crowd Simulation Model with Emotional Contagion and Evolutionary Game Theory [PDF]
Antagonistic crowd behaviors are often observed in cases of serious conflict. Antagonistic emotions, which is the typical psychological state of agents in different roles (i.e. cops, activists, and civilians) in crowd violent scenes, and the way they spread through contagion in a crowd are important causes of crowd antagonistic behaviors.
arxiv +1 more source
Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands [PDF]
Short chain fatty acids (SCFAs) are produced in the gut by bacterial fermentation of poorly digested carbohydrates. A key mediator of their actions is the G protein-coupled Free Fatty Acid 2 (FFA2) receptor and this has been suggested as a therapeutic ...
Hansen, Anders Højgaard+6 more
core +1 more source
Theory of partial agonist activity of steroid hormones
The different amounts of residual partial agonist activity (PAA) of antisteroids under assorted conditions have long been useful in clinical applications but remain largely unexplained.
Carson C. Chow+3 more
doaj +1 more source
Background and purpose: GPR35, a member of the orphan G-protein-coupled receptor, was recently implicated in colorectal cancer (CRC). However, whether targeting GPR35 by antagonists can inhibit its pro-cancer role has yet to be answered.Experimental ...
Wuxiyar Otkur+9 more
doaj +1 more source
Anti-nausea effects and pharmacokinetics of ondansetron, maropitant and metoclopramide in a low-dose cisplatin model of nausea and vomiting in the dog: a blinded crossover study [PDF]
Nausea is a subjective sensation which is difficult to measure in non-verbal species. The aims of this study were to determine the efficacy of three classes of antiemetic drugs in a novel low dose cisplatin model of nausea and vomiting and measure change
A Freeman+47 more
core +1 more source
BackgroundAndrogen deprivation therapy is the mainstay of medical treatment for prostate cancer (Pca); however, it is associated with an increased risk of adverse cardiovascular (CV) events and death.
Li Gu, Xurui Li, Wentao Liu
doaj +1 more source
Percolation on interacting, antagonistic networks [PDF]
Recently, new results on percolation of interdependent networks have shown that the percolation transition can be first order. In this paper we show that, when considering antagonistic interactions between interacting networks, the percolation process might present a bistability of the equilibrium solution.
arxiv +1 more source
Certaines propriétés des jeux à somme nulle sont étendues à différentes classes de jeux à deux joueurs à somme non nulle. Les définitions de ces classes sont basées sur différentes notions d'antagonisme. La notion de jeux presque strictement compétitifs, introduite par Aumann en 1961, est généralisée en gardant l'unicité du paiement d'équilibre de Nash.
openaire +2 more sources