Browse Items · NEOMED Bibliography Database

Discriminative stimulus properties of CGS 9896: interactions within the GABA/benzodiazepine receptor complex.

Male rats were trained to discriminate the stimulus effects of CGS 9896 (30.0 mg/kg) from its vehicle. Once trained, discriminative performance was observed to be dose-responsive in the 3.75-30.0 mg/kg range and analysis of the dose-response curve…

A subtherapeutic international normalized ratio despite increasing doses of warfarin: could this be malabsorption?

OBJECTIVE: To describe a case of warfarin resistance apparently caused by malabsorption and to review the literature regarding warfarin resistance. CASE SUMMARY: A 28-year-old renal transplant patient with systemic lupus erythematosus was admitted…

Biphasic effects of ethanol tested with drug discrimination in HAD and LAD rats.

Seventh-generation selectively bred high-alcohol-drinking (HAD) and low-alcohol-drinking (LAD) rats were trained to make differential responses for ethanol (0.75 g/kg, IP) and saline vehicle, following postadministration intervals (PI) of 2 min…

Tags: 1992, Alcohol Drinking/genetics/*psychology, Animals, Discrimination (Psychology)/*drug effects, Discrimination Learning/drug effects, Dose-Response Relationship, Drug, Ethanol/*pharmacology, Inbred Strains, Krimmer E C, Male, Pentobarbital/pharmacology, Pharmacology, biochemistry, and behavior, Rats, Serotonin Antagonists/pharmacology, Sleep/drug effects, Time Factors, Tropanes/pharmacology

Evaluation of factors associated with achieving glycemic control in a pharmacist-managed diabetes clinic.

The aim of this study was to identify factors that are associated with patients achieving goal A1c after 6 months in a pharmacist-managed diabetes clinic. This study is a descriptive, retrospective chart review of patients with type 2 diabetes…

Tags: 2014, Ambulatory Care, Ambulatory Care/organization & administration, American journal of therapeutics, Blood Glucose – Drug Effects, Blood Glucose/drug effects, Boros Melanie L, Department of Internal Medicine, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Diabetes Mellitus, Dose-Response Relationship, Drug, Female, Follow-Up Studies, Frazee Lawrence A, Glycated Hemoglobin A/metabolism, Glycosylated – Metabolism, Hemoglobin A, Human, Humans, Hypoglycemic Agents – Administration and Dosage, Hypoglycemic Agents – Therapeutic Use, Hypoglycemic Agents/administration & dosage/*therapeutic use, Insulin – Administration and Dosage, Insulin – Therapeutic Use, Insulin/administration & dosage/therapeutic use, Kostoff Matthew D, Male, Middle Age, Middle Aged, Moorman John M, NEOMED College of Medicine, NEOMED College of Pharmacy, Pharmaceutical Services/*organization & administration, Pharmacists – Administration, Pharmacists/*organization & administration, Pharmacy Service – Administration, Prospective Studies, Retrospective Design, Retrospective Studies, Social Work – Statistics and Numerical Data, Social Work/statistics & numerical data, Treatment Outcome, Treatment Outcomes, Type 2 – Drug Therapy, Type 2/*drug therapy

A lack of supersensitivity to opioid receptor agonists following chronic spinal opioid receptor antagonist administration in the rat.

1. Male Sprague-Dawley rats were chronically tested with intrathecal (i.t.) receptor selective opioid antagonists to determine if antinociceptive supersensitivity developed to selective i.t. opioid receptor agonists. 2. A subcutaneously implanted…

Activation of metabotropic glutamate receptor 1 dimers requires glutamate binding in both subunits.

Group I metabotropic glutamate receptors (mGluRs) form stable, disulfide-linked homodimers. Lack of a verifiably monomeric mGluR1 mutant has led to difficulty in assessing the role of dimerization in the molecular mechanism of mGluR1 activation. The…

Phase II study of gefitinib in patients with advanced salivary gland cancers.

BACKGROUND: The purpose of this study was to determine the antitumor activity of the epidermal growth factor receptor (EGFR) inhibitor gefitinib in patients with recurrent/metastatic salivary gland cancer. METHODS: We conducted a phase II study in…

Tags: 2015, 80 and over, Adenocarcinoma/drug therapy/mortality/pathology, adenoid cystic carcinoma, Adenoid Cystic/*drug therapy/mortality/pathology, Adult, Aged, Antineoplastic Agents/*therapeutic use, Blumenschein George R Jr, Carcinoma, Department of Internal Medicine, Disease-Free Survival, Dose-Response Relationship, Drug, Drug Administration Schedule, El-Naggar Adel K, Female, Gefitinib, Glisson Bonnie S, Gonzalez-Angulo Ana M, Head & neck, Humans, Jakob John A, Kies Merrill S, Kupferman Michael E, Lee J Jack, Liu Diane D, Local/*drug therapy/mortality/pathology, Male, Maximum Tolerated Dose, Middle Aged, NEOMED College of Medicine, Neoplasm Invasiveness/pathology, Neoplasm Recurrence, Neoplasm Staging, non-adenoid cystic carcinoma, Prognosis, Quinazolines/*therapeutic use, Remission Induction, response to therapy, salivary gland cancer, Salivary Gland Neoplasms/*drug therapy/mortality/pathology, Survival Analysis, Treatment Outcome

Acute exercise attenuates phenylephrine-induced contraction of rabbit isolated aortic rings.

Factors associated with a single bout of dynamic exercise (increased circulating catecholamines, increased body temperature, and decreased pH) are known to attenuate the vascular response to alpha-adrenergic receptor activation. Therefore, we…

Reduced vascular responsiveness after a single bout of dynamic exercise in the conscious rabbit.

We measured agonist-induced changes in the iliac artery blood flow velocity (IFV) independent of baroreflex-mediated compensatory mechanisms in chronically instrumented New Zealand White rabbits (n = 8). Animals were instrumented with a Doppler flow…

Pyrethroid Insecticides Directly Activate Microglia Through Interaction With Voltage-Gated Sodium Channels.

Microglia are considered to be the resident immune cells of the central nervous system and contribute significantly to ongoing neuroinflammation in a variety of neurodegenerative diseases. Recently, we and others identified that voltage-gated sodium…

The effect of immediate intraperitoneal carboplatinum on wound healing.

The effect of introducing intraperitoneal carboplatinum on wound healing immediately after wound closure was studied using a rat model. All animals were opened through a midline incision. A bowel anastomosis was then performed in a single-or…

Tags: 1993, Animals, Carboplatin/*administration & dosage/pharmacology, Clark T, Dose-Response Relationship, Drug, Gynecologic oncology, Hopkins M P, Injections, Intraperitoneal, Jenison E L, Male, Postoperative Period, Rats, Shellhaas C, Sprague-Dawley, Stakleff K S, Tissue Adhesions/etiology, Wound Healing/*drug effects

In Vivo Pharmacokinetics And Biodistribution Of Novel All-trans Retinoic Acid Derivative-loaded, Folate-modified Poly (l-amino Acid) Micelles

Folate is widely used as a target ligand for tumor cells, and poly (L-aspartic acid)-b-poly-(L-phenylalanine) (PAA-PPA) is a biodegradable material with low immunogenicity and toxicity. In this study, to enhance the targeting effect,…

Valproate increases dopamine transporter expression through histone acetylation and enhanced promoter binding of Nurr1.

The dopamine transporter (DAT) is the key regulator of dopaminergic transmission and is a target of several xenobiotics, including pesticides and pharmacological agents. Previously, we identified a prominent role for histone deacetylases in the…

Tags: 2017, Acetylation/drug effects, Animals, Butyrates/pharmacology, Cell Line, Cell Survival/drug effects, Department of Pharmaceutical Sciences, Dopamine Plasma Membrane Transport Proteins/*metabolism, Dopamine transporter, Dopaminergic Neurons/cytology/drug effects/metabolism, Dose-Response Relationship, Drug, Eid Aseel, Epigenesis, Epigenetics, Genetic, Genetic/drug effects, Green Ashley L, Group A, Guo Grace L, HDAC, Histone deacetylase, Histone Deacetylase Inhibitors/*pharmacology, Histone Deacetylases/metabolism, Histones/*drug effects/metabolism, Homeodomain Proteins/metabolism, Hydroxamic Acids/pharmacology, Member 2/*metabolism, Messenger/metabolism, NEOMED College of Pharmacy, Neuropharmacology, Nuclear Receptor Subfamily 4, Nurr1, Pitx3, Promoter Regions, Rats, Richardson Jason R, RNA, Transcription Factors/metabolism, Valproate, Valproic Acid/*pharmacology, Zarbl Helmut, Zhan Le

Structure-based design of a thiazolidinedione which targets the mitochondrial protein mitoNEET.

Several PPAR-gamma agonists containing a thiazolidinedione moiety (referred to as glitazones) have been proposed to be neuroprotective and appear to alter mitochondrial function. Recently, a search for mitochondrial proteins that bind pioglitazone…

A novel binding assay identifies high affinity ligands to the rosiglitazone binding site of mitoNEET.

A novel outer mitochondrial membrane protein containing [2Fe-2S] clusters, mitoNEET was first identified through its binding to the anti-diabetic drug pioglitazone. Pioglitazone belongs to a family of drugs that are peroxisome proliferator-activated…

Tags: 2011, Awale Prabha S, Binding Sites/drug effects, Bioorganic & medicinal chemistry letters, Carroll Richard T, Dose-Response Relationship, Drug, Funk Max O, Geldenhuys Werner J, Ligands, Lin Li, Mitochondrial Proteins/*antagonists & inhibitors/metabolism, Molecular Structure, Recombinant Proteins/antagonists & inhibitors/metabolism, Rosiglitazone, Stereoisomerism, Structure-Activity Relationship, Thiazolidinediones/chemical synthesis/chemistry/*pharmacology

Structure-activity and in vivo evaluation of a novel lipoprotein lipase (LPL) activator.

Elevated triglycerides (TG) contribute towards increased risk for cardiovascular disease. Lipoprotein lipase (LPL) is an enzyme that is responsible for the metabolism of core triglycerides of very-low density lipoproteins (VLDL) and chylomicrons in…

Solutions to the problem of bacterial resistance.

The recent increase in bacterial resistance has been, and continues to be, unmatched by drug discovery and development. The judicious use of antibacterials must be observed so as to contain bacterial resistance and maintain the utility of agents…

Tags: *Drug Resistance, *Practice Guidelines as Topic, 2005, Anti-Bacterial Agents/*therapeutic use, Bacterial, Department of Internal Medicine, Dose-Response Relationship, Drug, Drug Administration Schedule, Drug Prescriptions/standards, Drug Utilization, File Thomas M Jr, Humans, NEOMED College of Medicine, Professional Practice/*standards, Treatments in respiratory medicine, Unnecessary Procedures

Time and dose dependency of the suppression of pulmonary metastases of rat mammary cancer by amiloride.

Amiloride is an inhibitor of urokinase plasminogen activator (uPA), an essential component of the plasminogen/plasmin enzyme system. Inhibition of uPA prevents the conversion of plasminogen to tumor cell surface bound plasmin which is required for…

Sex differences in extracellular and intracellular calcium-mediated vascular reactivity to vasopressin in rat aorta.

In rat thoracic aorta, contractile responses to arginine vasopressin are two-fold higher in females than in males. To determine the roles of extracellular and intracellular Ca2+ in this sexual dimorphism in vascular function, vascular reactivity and…

Resveratrol inhibition of varicella-zoster virus replication in vitro.

Resveratrol was found to inhibit varicella-zoster virus (VZV) replication in a dose-dependent and reversible manner. This decrease in virus production in the presence of resveratrol was not caused by direct inactivation of VZV or inhibition of virus…

Resveratrol inhibition of Propionibacterium acnes.

OBJECTIVES: To evaluate the effects of the anti-inflammatory hydroxystilbene, resveratrol, on Propionibacterium acnes growth. METHODS: Three different strains of P. acnes were tested against resveratrol at concentrations between 0 and 200 mg/L.…

Pertubation of beta1 integrin function using anti-sense or function-blocking antibodies on corneal cells grown on fibronectin and tenascin.

During corneal development, neural crest derivatives from the periocular mesenchyme migrate into the cornea and differentiate into corneal fibroblasts. During this time, these cells interact with a variety of extracellular matrices for proper…

The effect of gender and the neurotrophin, BDNF, upon methamphetamine-induced neurotoxicity of the nigrostriatal dopaminergic system in mice.

The interactive effects between gender and a selective alteration in the neurotrophin, brain-derived neurotrophic factor (BDNF) upon methamphetamine (MA)-induced neurotoxicity of the nigrostriatal dopaminergic (NSDA) system were assessed. MA…

The effects of nicotine on dopamine and DOPAC output from rat striatal tissue.

The effects of varying doses of nicotine infusion upon spontaneous (basal) and subsequent potassium chloride-stimulated dopamine and 3,4-dihydroxyphenylacetic acid (DOPAC) output from superfused corpus striatal tissue fragments of male rats were…

Tags: 1998, 3, 4-Dihydroxyphenylacetic Acid/*metabolism, Amphetamine/pharmacology, Anderson L I, Animals, Central Nervous System Stimulants/pharmacology, Corpus Striatum/*drug effects/*metabolism, Dluzen D E, Dopamine/*metabolism, Dose-Response Relationship, Drug, European journal of pharmacology, Ganglionic Stimulants/administration & dosage/*pharmacology, Male, Nicotine/administration & dosage/*pharmacology, Potassium Chloride/pharmacology, Rats, Sprague-Dawley

Vagal afferents reflexly inhibit exercise in conscious rats.

Activation of vagal afferents reflexly inhibited locomotion induced by stimulation of the mesencephalic locomotor region in decerebrate cats. However, this reflex has not been tested in intact mammals. Therefore, the purpose of this study was to test…

Effect of a standardized pharyngitis treatment protocol on use of antibiotics in a pediatric emergency department.

BACKGROUND: Pharyngitis is a common complaint in pediatric patients. If clinical parameters are used alone, bacterial pathogens will be wrongly implicated in many cases. A nonstandardized approach to the treatment of children with pharyngitis in an…

Rotenone produces opposite effects upon mouse striatal dopamine function as a result of environmental temperature.

Rotenone is a commonly used pesticide that can function as an environmental neurotoxin. Rotenone is a known mitochondrial complex I inhibitor which can lead to oxidative stress and results in dopaminergic cell death. Another environmental factor…

Tags: *temperature, 2006, 3, 4-Dihydroxyphenylacetic Acid/metabolism, Analysis of Variance, Animals, Brain Chemistry/drug effects/physiology/radiation effects, Corpus Striatum/*drug effects/metabolism, Crutchfield Karla C, Dluzen Dean E, Dopamine/*metabolism, Dose-Response Relationship, Drug, Insecticides/*pharmacology, Methamphetamine/pharmacology, Mice, Neurotoxicity research, Rotenone/*pharmacology

Serotonin contributes to the spinal antinociceptive effects of morphine.

This study was designed to determine if morphine administered intrathecally (IT) interacts with serotonergic or noradrenergic nerve terminals in the spinal cord to produce analgesia on the spinally mediated tail-flick test. Male Sprague-Dawley rats…

Age-related changes in the spinal antinociceptive effects of DAGO, DPDPE and beta-endorphin in the rat.

These studies were designed to investigate how the aging process alters the spinal antinociceptive efficacy of mu (mu), delta (delta) and epsilon (epsilon) opioid receptor agonists administered intrathecally (i.t.) in rats. Various doses of the mu…

Effects of aging on spinal opioid-induced antinociception.

Initial experiments were conducted to determine whether or not the aging process alters the ability of young, mature, or aged male Fischer 344 rats (5- to 6-, 15- to 16-, and 25- to 26-months-old, respectively) to respond to thermal nociceptive…

The antinociceptive effects of 3,4-methylenedioxymethamphetamine (MDMA) in the rat.

The antinociceptive effects of MDMA and morphine were examined in rats using the tail-flick and hot-plate analgesiometric tests. MDMA, in the dose range of 1.5-6.0 mg/kg IP, produced a dose-dependent elevation in hot-plate latency, but did not…

Testosterone causes direct relaxation of rat thoracic aorta.

Several recent studies have provided evidence that gonadal steroid hormones can exert acute (nongenomic) effects on both neural and vascular tissues. This study examines the acute effects of testosterone (T) on vascular reactivity of the rat thoracic…

Regulation of human sterol 27-hydroxylase gene (CYP27A1) by bile acids and hepatocyte nuclear factor 4alpha (HNF4alpha).

Mitochondrial sterol 27-hydroxylase (CYP27A1) catalyses sterol side-chain oxidation of bile acid synthesis from cholesterol, and the first reaction of the acidic bile acid biosynthetic pathway. Hydrophobic bile acids suppress human CYP27A1 gene…

Tags: *DNA-Binding Proteins, 2003, Base Sequence, Basic Helix-Loop-Helix Leucine Zipper Transcription Factors, Bile Acids and Salts/*pharmacology, Binding Sites/genetics, Cell Line, Chen Wenling, Chenodeoxycholic Acid/pharmacology, Chiang John Y L, Cholestanetriol 26-Monooxygenase, Cloning, Cultured, Cytoplasmic and Nuclear/genetics/metabolism, Department of Integrative Medical Sciences, DNA, DNA/chemistry/genetics, Dose-Response Relationship, Drug, gene, Gene Expression Regulation/drug effects, Genetic/*genetics, Hepatocyte Nuclear Factor 4, Humans, Luciferases/genetics/metabolism, Molecular, Molecular Sequence Data, Mutagenesis, Mutation, NEOMED College of Medicine, Phosphoproteins/genetics/*metabolism, Promoter Regions, Receptors, Recombinant Fusion Proteins/genetics/metabolism, Response Elements/genetics, Sequence Analysis, Site-Directed, Steroid Hydroxylases/*genetics, Transcription Factors/genetics/*metabolism, Transfection, Tumor Cells

Preferential increase in pituitary prolactin versus vasoactive intestinal peptide as a function of estradiol benzoate dose in the ovariectomized rat.

Vasoactive intestinal peptide (VIP) is synthesized in various tissues, including the anterior pituitary gland, where it may stimulate the release of PRL. Because estrogen plays a central role in the regulation of PRL, it becomes important to…

Calcium channel blockade attenuates angiotensin II-induced drinking in rats.

Lateral ventricular administration of angiotensin II (ANG II) produces potent dipsogenic effects in water-sated rats. ANG II seems to require functional voltage-gated calcium channels on neurons throughout circumventricular brain sites to exert its…

Tags: 1993, Amino Acid Sequence, Angiotensin II/*antagonists & inhibitors/pharmacology, Animals, Brain research bulletin, Calcagnetti D J, Calcium Channel Blockers/administration & dosage/*pharmacology, Dimethyl Sulfoxide/pharmacology, Dose-Response Relationship, Drinking Behavior/*drug effects, Drug, Injections, Intraventricular, Isradipine/pharmacology, Male, Molecular Sequence Data, Rats, Schechter M D, Sprague-Dawley

Attenuation of drinking sweetened water following calcium channel blockade.

Recent reports cite results that both cocaine-induced conditioned place preference and activity stimulation are attenuated by pretreatment with the calcium channel blocker isradipine (ISR) in rats. By blocking voltage-dependent

Increases in the locomotor activity of rats after intracerebral administration of cathinone.

There is a widespread practice among people living in Eastern Africa and Southern Arabia of chewing the leaves of the Khat shrub so as to produce pharmacological effects that are practically indistinguishable from those produced by amphetamine…

Tags: 1992, Alkaloids/administration & dosage/*pharmacology, Animals, Brain research bulletin, Calcagnetti D J, Cerebral Ventricles/drug effects/*physiology, Dose-Response Relationship, Drug, Injections, Intraventricular, Male, Motor Activity/*drug effects, Nucleus Accumbens/drug effects/*physiology, Psychotropic Drugs/administration & dosage/*pharmacology, Rats, Schechter M D, Sprague-Dawley, Stereotaxic Techniques, Substantia Nigra/drug effects/*physiology

Place preference for the psychostimulant cathinone is blocked by pretreatment with a dopamine release inhibitor.

1. The objective of Exp. 1 was to determine whether intracerebroventricular (ICV) injection of cathinone CATH (8.0-32 micrograms) would produce a dose-dependent conditioned place preference (CPP) and/or activation in rats. Results indicate that rats…

Antiepileptics inhibit cortical N-methyl-D-aspartate-evoked [3H]norepinephrine efflux.

The antiepileptic drugs phenytoin, valproic acid and phenobarbital were examined for their ability to inhibit N-methyl-D-aspartate (NMDA)-stimulated [3H]norepinephrine efflux from rat brain cortical slices. All three drugs inhibited efflux at varying…

Tags: 1994, Animals, Anticonvulsants/*pharmacology, Brown L M, Dose-Response Relationship, Drug, European journal of pharmacology, Female, Lee Y P, Male, N-Methylaspartate/*antagonists & inhibitors, Norepinephrine/*metabolism, Rats, Teyler T J

Myocardial work load is a major determinant of norepinephrine-induced left ventricular dysfunction.

This study was conducted to determine whether increased myocardial energy demand plays a role in norepinephrine (NE)-induced left ventricular (LV) dysfunction. A range of arterial pressure-heart rate (P-R) products (myocardial energy demand) was…

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