which drugs can interact: enzymes (e.g. neostigmine and acetyl cholinesterase), membrane carriers (e.g. tricyclic antidepressants and catecholamine uptake-1), ion channels (e.g. nimodipine and voltage-gated Ca2þ channels) and receptors. This article is concerned with the receptor and describes the dynamics of drug–receptor interaction, agonists, antagonists, partial agonists and inverse agonist...

introduction: the neuroprotective role of opioid morphine against 6-hydroxydopamineinduced cell death has been demonstrated. however, the exact mechanism(s) underlying such neuroprotection, especially the role of subtype receptors, has not yet been fully clarified. methods: here, we investigated the effects of different opioid agonists on 6-ohda-induced neurotoxicity in human neuroblastoma sh-s...

Recent years have witnessed the discovery of novel selective agonists of the M(1) muscarinic acetylcholine (ACh) receptor (mAChR). One mechanism invoked to account for the selectivity of such agents is that they interact with allosteric sites. We investigated the molecular pharmacology of two such agonists, 1-[3-(4-butyl-1-piperidinyl)propyl]-3,4-dihydro-2(1H)-quinolinone (77-LH-28-1) and 4-n-b...

Most of the currently available G protein-coupled receptor (GPCR) crystal structures represent an inactive receptor state, which has been considered to be suitable only for the discovery of antagonists and inverse agonists in structure-based computational ligand screening. Using the β(2)-adrenergic receptor (B2AR) as a model system, we show that a dynamic homology model based on an "active" ops...

Introduction Studies consistently show that patients with prescription opioid use disorder (OUD) respond to buprenorphine treatment. Few studies have followed these in the long-term. Our longitudinal research has shown abstinence be associated most strongly agonist/partial agonist We also found many used treatment inconsistently; questions remain about benefits of intermittent Objectives examin...

The Aim. current study evaluates the possibility of using C646G polymorphic variant NR3C1 gene (rs41423247) for personalized administration combination therapy with inhaled glucocorticosteroids (iGCs) and long-acting β2-agonists in patients asthma/COPD overlap (ACO) without obesity.Material methods. Forty ACO were included (17 BMI < 30 23 obesity (BMI ≥ 30) to received combined treatment use...

BACKGROUND We previously showed that growth hormone-releasing hormone (GHRH) agonists are cardioprotective following myocardial infarction (MI). Here, our aim was to evaluate the in vitro and in vivo activities of highly potent new GHRH agonists, and elucidate their mechanisms of action in promoting cardiac repair. METHODS AND RESULTS H9c2 cells were cultured in serum-free medium, mimicking n...

Some of the most compelling evidence supporting an association between cannabinoid agonists and psychosis comes from controlled laboratory studies in humans. Randomized, double-blind, placebo-controlled, crossover laboratory studies demonstrate that cannabinoid agonists, including phytocannabinoids and synthetic cannabinoids, produce a wide range of positive, negative, and cognitive symptoms an...

[3H]Quisqualic acid (QA) was synthesized and used to label metabotropic glutamate receptor (mGluR) in rat brain synaptic membranes in the presence of three different ionotropic glutamate receptor agonists at respective saturating concentrations. Of several mGluR agonists tested, group I agonists were more potent in displacing [3H]QA binding than group II and group III agonists in the presence o...

Glucagon-like peptide-1, produced predominantly in enteroendocrine cells, controls glucose metabolism and energy homeostasis through regulation of islet hormone secretion, gastrointestinal motility, and food intake, enabling development of GLP-1 receptor (GLP-1R) agonists for the treatment of diabetes and obesity. GLP-1 also acts on the immune system to suppress inflammation, and GLP-1R signali...