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A Statement on the Pharmacology of Reinstatement: Naltrexone and Relapse to Opioid Seeking [Viewpoint]
A Statement on the Pharmacology of Reinstatement: Naltrexone and Relapse to Opioid Seeking [Viewpoint]
This issue of the Journal of Pharmacology and Experimental Therapeutics includes an article by Withey et al. that addresse...
The Effects of Chronic Naltrexone on Reinstatement of Opioid-Induced Drug-Seeking Behavior and Antinociception [Behavioral Pharmacology]
The Effects of Chronic Naltrexone on Reinstatement of Opioid-Induced Drug-Seeking Behavior and Antinociception [Behavioral Pharmacology]
AbstractOpioid addiction is a chronic relapsing disorder in which drug-seeking behavior during abstinence can be provoked ...
Label-Free Dynamic Mass Redistribution Assay To Characterize Holistic Chemokine Receptor Pharmacology in Neutrophils [Viewpoint]
Label-Free Dynamic Mass Redistribution Assay To Characterize Holistic Chemokine Receptor Pharmacology in Neutrophils [Viewpoint]
In a study published in this issue of JPET, Stott et al. (2024) investigated the capacity of the label-free dynamic mass r...
The Neutrophil Dynamic Mass Redistribution Assay as a Medium throughput Primary Cell Screening Assay [Drug Discovery and Translational Medicine]
The Neutrophil Dynamic Mass Redistribution Assay as a Medium throughput Primary Cell Screening Assay [Drug Discovery and Translational Medicine]
AbstractIn a typical G protein coupled receptor drug discovery campaign, an in vitro primary functional screening assay is...
Obituary: Travis Thompson--Editorial [Editorial]
Obituary: Travis Thompson--Editorial [Editorial]
Dr. Travis Thompson, a pioneer in behavioral pharmacology and a leading innovator in behavioral medicine and developmental...
N-Acetylcysteine Alters Disease Progression and Increases Janus Kinase Mutation Frequency in a Mouse Model of Precursor B-Cell Acute Lymphoblastic Leukemia [Cellular and Molecular]
N-Acetylcysteine Alters Disease Progression and Increases Janus Kinase Mutation Frequency in a Mouse Model of Precursor B-Cell Acute Lymphoblastic Leukemia [Cellular and Molecular]
AbstractB-cell acute lymphoblastic leukemia (B-ALL) is the most prevalent type of cancer in young children and is associat...
Endothelial Extracellular Vesicles Enriched in microRNA-34a Predict New-Onset Diabetes in Coronavirus Disease 2019 (COVID-19) Patients: Novel Insights for Long COVID Metabolic Sequelae [Cardiovascular]
Endothelial Extracellular Vesicles Enriched in microRNA-34a Predict New-Onset Diabetes in Coronavirus Disease 2019 (COVID-19) Patients: Novel Insights for Long COVID Metabolic Sequelae [Cardiovascular]
AbstractEmerging evidence indicates that the relationship between coronavirus disease 2019 (COVID-19) and diabetes is 2-fo...
Development of Cilofexor, an Intestinally-Biased Farnesoid X Receptor Agonist, for the Treatment of Fatty Liver Disease [Drug Discovery and Translational Medicine]
Development of Cilofexor, an Intestinally-Biased Farnesoid X Receptor Agonist, for the Treatment of Fatty Liver Disease [Drug Discovery and Translational Medicine]
AbstractThe farnesoid X receptor (FXR) is a nuclear receptor that controls bile acid, lipid, and cholesterol metabolism. F...
Lucanthone, a Potential PPT1 Inhibitor, Perturbs Stemness, Reduces Tumor Microtube Formation, and Slows the Growth of Temozolomide-Resistant Gliomas In Vivo [Chemotherapy, Antibiotics, and Gene Therapy]
Lucanthone, a Potential PPT1 Inhibitor, Perturbs Stemness, Reduces Tumor Microtube Formation, and Slows the Growth of Temozolomide-Resistant Gliomas In Vivo [Chemotherapy, Antibiotics, and Gene Therapy]
AbstractGlioblastoma (GBM) is the most frequently diagnosed primary central nervous system tumor in adults. Despite the st...
Humanization of SLCO2B1 in Rats Increases rCYP3A1 Protein Expression but Not the Metabolism of Erlotinib to OSI-420 [Metabolism, Transport, and Pharmacogenetics]
Humanization of SLCO2B1 in Rats Increases rCYP3A1 Protein Expression but Not the Metabolism of Erlotinib to OSI-420 [Metabolism, Transport, and Pharmacogenetics]
AbstractThe organic anion transporting polypeptide (OATP)2B1 [(gene: solute carrier organic anion transporter family membe...
Suppression of Mast Cell Activation by GPR35: GPR35 Is a Primary Target of Disodium Cromoglycate [Inflammation, Immunopharmacology, and Asthma]
Suppression of Mast Cell Activation by GPR35: GPR35 Is a Primary Target of Disodium Cromoglycate [Inflammation, Immunopharmacology, and Asthma]
AbstractMast cell stabilizers, including disodium cromoglycate (DSCG), were found to have potential as the agonists of an ...
NCP, a Dual Kappa and mu Opioid Receptor Agonist, Is a Potent Analgesic Against Inflammatory Pain without Reinforcing or Aversive Properties [Neuropharmacology]
NCP, a Dual Kappa and mu Opioid Receptor Agonist, Is a Potent Analgesic Against Inflammatory Pain without Reinforcing or Aversive Properties [Neuropharmacology]
AbstractWhile agonists of μ (MOR) and κ (KOR) opioid receptors have analgesic effects, they produce euphoria and dysphoria...
Pharmacokinetics of Panobinostat: Interspecies Difference in Metabolic Stability [Metabolism, Transport, and Pharmacogenetics]
Pharmacokinetics of Panobinostat: Interspecies Difference in Metabolic Stability [Metabolism, Transport, and Pharmacogenetics]
AbstractThe deregulation of histone deacetylase (HDAC) expression is often seen in many cancers, and HDAC inhibitors have ...
Correction to "The {beta}-Blocker Carvedilol and Related Aryloxypropanolamines Promote ERK1/2 Phosphorylation in HEK293 Cells with KA Values Distinct From Their Equilibrium Dissociation Constants as {beta}2-Adrenoceptor Antagonists: Evidence for Functional Affinity" [Erratum]
Correction to "The {beta}-Blocker Carvedilol and Related Aryloxypropanolamines Promote ERK1/2 Phosphorylation in HEK293 Cells with KA Values Distinct From Their Equilibrium Dissociation Constants as {beta}2-Adrenoceptor Antagonists: Evidence for Functional Affinity" [Erratum]
In the above article [Hamed O, Jayasinghe V, and Giembycz M (2024) J Pharmacol Exp Ther 388:688–700; DOI: https://doi.org/...
Selective KCNQ2/3 Potassium Channel Opener ICA-069673 Inhibits Excitability in Mouse Vagal Sensory Neurons [Neuropharmacology]
Selective KCNQ2/3 Potassium Channel Opener ICA-069673 Inhibits Excitability in Mouse Vagal Sensory Neurons [Neuropharmacology]
AbstractHeightened excitability of vagal sensory neurons in inflammatory visceral diseases contributes to unproductive and...
Is Overexpression of the Plasma Membrane Transporter (SLC29A4) a New Option to Stratify Patients with High-Risk Neuroblastoma for Treatment with 131I-mIBG? [Viewpoint]
Is Overexpression of the Plasma Membrane Transporter (SLC29A4) a New Option to Stratify Patients with High-Risk Neuroblastoma for Treatment with 131I-mIBG? [Viewpoint]
Neuroblastoma (NB) is a heterogenous disease with solid tumors in infants and young children originating from neural crest...
The Plasma Membrane Monoamine Transporter is Highly Expressed in Neuroblastoma and Functions as an mIBG Transporter [Metabolism, Transport, and Pharmacogenetics]
The Plasma Membrane Monoamine Transporter is Highly Expressed in Neuroblastoma and Functions as an mIBG Transporter [Metabolism, Transport, and Pharmacogenetics]
AbstractNeuroblastoma (NB) is a pediatric cancer with low survival rates in high-risk patients. 131I-mIBG has emerged as a...
Unlocking the Goldenseal Reveals the Complexities of Natural Product-Drug Interactions [Viewpoint]
Unlocking the Goldenseal Reveals the Complexities of Natural Product-Drug Interactions [Viewpoint]
Botanical natural products are a rich source of diverse phytochemicals that allow for the continued development of novel t...
An Integrative Approach to Elucidate Mechanisms Underlying the Pharmacokinetic Goldenseal-Midazolam Interaction: Application of In Vitro Assays and Physiologically Based Pharmacokinetic Models to Understand Clinical Observations [Metabolism, Transport, and Pharmacogenetics]
An Integrative Approach to Elucidate Mechanisms Underlying the Pharmacokinetic Goldenseal-Midazolam Interaction: Application of In Vitro Assays and Physiologically Based Pharmacokinetic Models to Understand Clinical Observations [Metabolism, Transport, and Pharmacogenetics]
AbstractThe natural product goldenseal is a clinical inhibitor of CYP3A activity, as evidenced by a 40%–60% increase in mi...
Role of Cannabinoid Signaling in Cardiovascular Function and Ischemic Injury [Minireview]
Role of Cannabinoid Signaling in Cardiovascular Function and Ischemic Injury [Minireview]
AbstractCardiovascular disease represents a leading cause of death, morbidity, and societal economic burden. The prevalenc...
Chidamide Induces Epstein-Barr Virus (EBV) Lytic Infection and Acts Synergistically with Tenofovir to Eliminate EBV-Positive Burkitt Lymphoma [Drug Discovery and Translational Medicine]
Chidamide Induces Epstein-Barr Virus (EBV) Lytic Infection and Acts Synergistically with Tenofovir to Eliminate EBV-Positive Burkitt Lymphoma [Drug Discovery and Translational Medicine]
1Blood Diseases Institute (L.X., M.Z., D.T., Z.L., T.L., Y.Z., S.Z., Y.M., D.Y., X.W., W.S.) and Key Laboratory of Bone Ma...
Serum Glucocorticoid-Regulated Kinase-1 in Ischemia-Reperfusion Injury: Blessing or Curse [Minireview]
Serum Glucocorticoid-Regulated Kinase-1 in Ischemia-Reperfusion Injury: Blessing or Curse [Minireview]
AbstractThe family of serum-glucocorticoid-regulated kinase (SGK) consists of three paralogs, SGK-1, SGK-2, and SGK-3, wit...
First-in-Human Phase 1 Randomized Trial with the Anti-CD40 Monoclonal Antibody KPL-404: Safety, Tolerability, Receptor Occupancy, and Suppression of T-Cell-Dependent Antibody Response [Inflammation, Immunopharmacology, and Asthma]
First-in-Human Phase 1 Randomized Trial with the Anti-CD40 Monoclonal Antibody KPL-404: Safety, Tolerability, Receptor Occupancy, and Suppression of T-Cell-Dependent Antibody Response [Inflammation, Immunopharmacology, and Asthma]
AbstractBlockade of the cluster of differentiation 40 (CD40)–CD40L interaction has potential for treating autoimmune disea...
Dimethyl Fumarate Ameliorated Cardiorenal Anemia Syndrome and Improved Overall Survival in Dahl/Salt-Sensitive Rats [Drug Discovery and Translational Medicine]
Dimethyl Fumarate Ameliorated Cardiorenal Anemia Syndrome and Improved Overall Survival in Dahl/Salt-Sensitive Rats [Drug Discovery and Translational Medicine]
IntroductionPatients with chronic kidney disease often develop cardiovascular disease and die before reaching end-stage re...
Biodistribution of Agmatine to Brain and Spinal Cord after Systemic Delivery [Neuropharmacology]
Biodistribution of Agmatine to Brain and Spinal Cord after Systemic Delivery [Neuropharmacology]
AbstractAgmatine, an endogenous polyamine, has been shown to reduce chronic pain behaviors in animal models and in patient...
Central Nervous System Distribution of Panobinostat in Preclinical Models to Guide Dosing for Pediatric Brain Tumors [Metabolism, Transport, and Pharmacogenetics]
Central Nervous System Distribution of Panobinostat in Preclinical Models to Guide Dosing for Pediatric Brain Tumors [Metabolism, Transport, and Pharmacogenetics]
AbstractAchieving adequate exposure of the free therapeutic agent at the target is a critical determinant of efficacious c...
Correction to "Could a Nebulized or Dry Powder Inhalation of a Dopamine D1R Agonist Be a Treatment of Idiopathic Pulmonary Fibrosis?" [Erratum]
Correction to "Could a Nebulized or Dry Powder Inhalation of a Dopamine D1R Agonist Be a Treatment of Idiopathic Pulmonary Fibrosis?" [Erratum]
In the above article, [Andresen B (2023) Could a Nebulized or Dry Powder Inhalation of a Dopamine D1R Agonist Be a Treatme...
A Novel Approach to Predicting Organic Anion Transporting Polypeptide Function in Human Hepatic Drug Disposition and Biliary Clearance [Viewpoint]
A Novel Approach to Predicting Organic Anion Transporting Polypeptide Function in Human Hepatic Drug Disposition and Biliary Clearance [Viewpoint]
The transport of drugs into and out of the liver plays a critical role in determining drug disposition and therapeutic eff...
Quantitative Prediction of OATP-Mediated Disposition and Biliary Clearance Using Human Liver Chimeric Mice [Drug Discovery and Translational Medicine]
Quantitative Prediction of OATP-Mediated Disposition and Biliary Clearance Using Human Liver Chimeric Mice [Drug Discovery and Translational Medicine]
AbstractDrug biliary clearance (CLbile) in vivo is among the most difficult pharmacokinetic parameters to predict accurate...
Hydrocodone, Oxycodone, and Morphine Metabolism and Drug-Drug Interactions [Minireview]
Hydrocodone, Oxycodone, and Morphine Metabolism and Drug-Drug Interactions [Minireview]
AbstractAwareness of drug interactions involving opioids is critical for patient treatment as they are common therapeutics...
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