Both entecavir and crizotinib are substrates of organic cation transporter 2 (OCT2). The aim of present study was to investigate the mechanisms of drug interactions between these two drugs. Kinetic […]» Read more
Essential role of STAT-3 dependent NF-κB activation on IL-6-mediated downregulation of hepatic transporters.
IL-6 markedly decreases the expression of numerous hepatic transporters. We previously demonstrated that IL-6-mediated downregulation of transporters occurs through STAT3, with partial involvement of PXR. However, while IL-6-mediated induction of […]» Read more
Pharmacokinetic profile of N-acetylcysteine amide and its main metabolite in mice using new analytical method.
N-acetylcysteine amide (NACA) is the amide derivative of N-acetylcysteine (NAC) that is rapidly converted to NAC after systemic administration. It has emerged as a promising thiol antioxidant for multiple indications; […]» Read more
The impact of dopamine D2-like agonist/antagonist on [18F]VAT PET measurement of VAChT in the brain of nonhuman primates.
Vesicular acetylcholine transporter (VAChT) is a promising target for a PET measure of cholinergic deficits which contribute to cognitive impairments. Dopamine D2-like agonists and antagonists are frequently used in the […]» Read more
Incarcerated patients often have a high disease burden and poor access to care in the community. In an effort to ensure glycemic control and appropriate initiation of statin therapy for […]» Read more
The first clinically relevant reports of St. John’s wort (SJW) interacting with drugs, altering their bioavailability and efficacy, were published around millennium: In 2000, a pharmacokinetic interaction between SJW and […]» Read more
Neuromuscular blockade (NMB) with cisatracurium may improve outcomes in the acute respiratory distress syndrome (ARDS) population; however, optimal dosing strategy remains unknown. Factors affecting pharmacokinetics and pharmacodynamics of cisatracurium may […]» Read more
We previously demonstrated that acetaminophen (AcAP) has to be metabolized in the brain by fatty acid amide hydrolase enzyme (FAAH) into AM404 (N-(4-hydroxyphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide) to recruit CB1 and TRPV1 receptors, responsible […]» Read more
Berberine protects against diabetic kidney disease via promoting PGC-1α-regulated mitochondrial energy homeostasis.
Lipid metabolism disorder and disturbed mitochondrial bioenergetics play pivotal roles in the occurrence and development of diabetic kidney disease (DKD). Berberine (BBR) is a kind of alkaloid derived from Chinese […]» Read more
Newly incarcerated inmates with chronic alcohol use are at high risk for alcohol withdrawal. This descriptive study aims to describe the role of a clinical pharmacist within an alcohol detoxification […]» Read more
Assessment of the Impact of Clinical Pharmacology Consultations Provided to Hospital Clinicians From the Drug Information Center-An Outcome Research in a Developing Country.
Drug Information Center (DIC) with on-call evidence-based medicine service can revolutionize health-care practice and also can play a major role in health-care delivery in both developed and developing countries.To assess […]» Read more
Enhancement of intestinal absorption of coenzyme Q10 using emulsions containing oleyl polyethylene acetic acids.
Emulsions have often been prepared to improve absorption of lipophilic compounds that have poor solubility. Coenzyme Q10 (CoQ10) is a lipophilic compound that has been used as an anti-aging supplement. […]» Read more
Novel neuroactive steroid with hypnotic and T-channel blocking properties exerts effective analgesia in a rodent model of post-surgical pain.
Neuroactive steroid (3β,5β,17β)-3-hydroxyandrostane-17-carbonitrile (3β-OH) is a novel hypnotic and voltage-dependent blocker of T-type calcium channels. Here we examine its potential analgesic effects and adjuvant anesthetic properties using a post-surgical pain […]» Read more
ANNEXIN-A1 DEFICIENCY EXACERBATES PATHOLOGICAL REMODELLING OF THE MESENTERIC VASCULATURE IN INSULIN-RESISTANCE BUT NOT INSULIN-DEFICIENCY.
Arterial stiffness, a hallmark of diabetes, increases the risk of cardiovascular complications. Potential mechanisms that promote arterial stiffness in diabetes include oxidative stress, glycation and inflammation. The anti-inflammatory protein annexin-A1 […]» Read more
The nociceptin/orphaninFQ receptor system as a target to alleviate cancer-induced bone pain in rats: Model validation and pharmacological evaluation.
Cancer-induced bone pain remains inadequately controlled and current standard of care analgesics are accompanied by several side effects. Nociceptin/orphanin FQ peptide (NOP) receptor agonists have demonstrated broad analgesic properties in […]» Read more
Carboxylesterase (CES) 1, CES2, and arylacetamide deacetylase (AADAC) are the major drug hydrolases in humans, and they have different substrate preferences. Because rodents are widely used in preclinical studies, we […]» Read more
PO-322 has potent immunosuppressive activity in vitro and in vivo by selectively inhibiting SGK1 activity.
Immunosuppressive drugs have shown great promise in treating the autoimmune diseases in recent years. A series of novel oxazole derivatives were screened for their immunosuppressive activity. PO-322 [1H-indole-2,3-dione 3-(1,3-benzoxazol-2-ylhydrazone)] was […]» Read more
Evaluation of current regulation and guidelines of pharmacogenomic drug labels; opportunities for improvements.
Pharmacogenomic drug labels in summary of product characteristics (SmPCs) provide an instrument for clinical implementation of pharmacogenomics. We compared pharmacogenomic guidance by CPIC, DPWG, FDA, and by the European agencies […]» Read more
PI3K-δ controls endoplasmic reticulum membrane fluidity and permeability in fungus-induced allergic inflammation.
Phosphoinositol 3-kinase (PI3K)-especially PI3K-δ-and endoplasmic reticulum (ER) stress play important roles in refractory asthma induced by the fungus Aspergillus fumigatus (Af) through mechanisms that are not well understood. This was […]» Read more
Acid-sensing ion channels blockade attenuates pressor and sympathetic responses to skeletal muscle metaboreflex activation in humans.
In animals, the blockade of acid-sensing ion channels (ASICs), cation pore-forming membrane proteins located in the free nerve endings of group IV afferent fibers, attenuates increases in arterial pressure (AP) […]» Read more
Human tridimensional neuronal cultures for phenotypic drug screening in inherited peripheral neuropathies.
Length-dependent axonal degeneration is the pathologic hallmark of several neurodegenerative disorders, including inherited peripheral neuropathies (Charcot-Marie-Tooth disease, CMT). CMT is currently an untreatable disorder. This is partially due to lack […]» Read more
Association of statin and its lipophilicity with cardiovascular events in patients receiving chronic dialysis.
Lipophilicity of statins has been linked to extrahepatic cells penetration and inhibition of isoprenoid synthesis and coenzyme Q10 which may affect myocardial contraction. Whether statins lipophilicity affects the risk of […]» Read more
NOP receptor antagonism reduces alcohol drinking in male and female rats through mechanisms involving the central amygdala and ventral tegmental area.
Click here to read the full article @ British journal of pharmacology» Read more
Association between the timing of consultation-liaison psychiatry interventions and the length of stay in general hospital.
Psychiatric comorbidities are frequent in patients admitted in general hospital and are associated with greater lengths of stay (LOS). Early consultation-liaison psychiatry (CLP) interventions may reduce the LOS but previous […]» Read more
Physiologically Based pharmacokinetic (PBPK) modeling for optimal dosage prediction of quinine co-administered with ritonavir-boosted lopinavir.
The co-formulated lopinavir/ritonavir significantly reduces quinine concentration in healthy volunteers due to potential drug-drug interactions (DDIs). However, DDIs information in malaria and HIV co-infected patients are lacking. The objective of […]» Read more
The mental health of children and young people can be disproportionally affected and easily overlooked in the context of emergencies and disasters. Child and adolescent mental health services can contribute […]» Read more
β3 adrenoceptor-induced cholinergic bladder inhibition involves EPAC1 and PKC favoring ENT1-mediated adenosine outflow from the human and rat detrusor.
The way β3 receptor agonists (e.g. mirabegron) control bladder overactivity may involve adenosine release from human and rat detrusor smooth muscle. Retrograde activation of adenosine A1 receptors reduces acetylcholine (ACh) […]» Read more
Randomized controlled trials are the gold standard to investigate efficacy and safety of new treatments. In certain settings, however, randomizing patients to control may be difficult for ethical or feasibility […]» Read more
Fifty years ago the BJP published the text of the Second Gaddum Lecture, given by John Vane to the British Pharmacological Society. This article assesses the origins of the experiments […]» Read more
Five diagnostic criteria sets for pathological grief are currently used in research. Studies evaluating their performance indicate that it is not justified to generalise findings regarding prevalence rates and predictive […]» Read more