Browse Items · NEOMED Bibliography Database

3D-QSAR and docking studies of pentacycloundecylamines at the sigma-1 (sigma1) receptor.

Pentacycloundecylamine (PCU) derived compounds have been shown to be promising lead structures for the development of novel drug candidates aimed at a variety of neurodegenerative and psychiatric diseases. Here we show for the first time a 3D…

Tags: *Quantitative Structure-Activity Relationship, 2013, Amines/*chemistry/metabolism, Aza Compounds/chemistry, Binding Sites, Bioorganic & medicinal chemistry letters, Geldenhuys Werner J, Kinetics, Malan Sarel F, Molecular Docking Simulation, Novotny Nicholas, Protein Binding, Protein Structure, Receptors, sigma/*chemistry/metabolism, Tertiary, Van der Schyf Cornelis J

3D-QSAR and docking studies on transforming growth factor (TGF)-beta receptor 1 antagonists.

The transforming growth factor-beta (TGF-beta) is part of a family of cytokines which regulate various signaling pathways such as cell development, growth, and tissue injury. Although several studies have been published describing the synthesis of…

Tags: 2010, Bioorganic & medicinal chemistry letters, Geldenhuys Werner J, Models, Molecular, Nakamura Hiroshi, Quantitative Structure-Activity Relationship, Receptors, Transforming Growth Factor beta/*antagonists & inhibitors

3D-Quantitative structure-activity relationship and docking studies of the tachykinin NK3 receptor.

The tachykinin NK(3) receptor (NK(3)R) is a novel drug target for schizophrenia and drug abuse. Since few non-peptide antagonists of this G protein-coupled receptor are available, we have initiated this study to gain a better understanding of the…

Tags: *Quantitative Structure-Activity Relationship, 2011, Binding Sites, Bioorganic & medicinal chemistry letters, Computer Simulation, Drug Design, Geldenhuys Werner J, Humans, Ligands, Models, Molecular, Neurokinin-3/*chemistry/metabolism, Protein Structure, Quinolines/chemistry, Receptors, Simmons Mark A, Tertiary

A comparative analysis of monoaminergic involvement in the spinal antinociceptive action of DAMPGO and DPDPE.

The antinociceptive properties of intrathecally (i.t.) administered [D-Ala2,

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…

A metabolic stress-inducible miR-34a-HNF4alpha pathway regulates lipid and lipoprotein metabolism.

Non-alcoholic fatty liver disease (NAFLD) is one of the most common liver diseases, but its underlying mechanism is poorly understood. Here we show that hepatocyte nuclear factor 4alpha (HNF4alpha), a liver-enriched nuclear hormone receptor, is…

A neurochemical heterogeneity of the rat striatum as measured by in vivo electrochemistry and microdialysis.

The neurochemical heterogeneity of the rat striatum was assessed in vivo by measuring subregional changes in extracellular dopamine and DOPAC by in vivo electrochemistry and microdialysis in response to amphetamine and the D2 antagonist,…

Tags: 1990, 3, 4-Dihydroxyphenylacetic Acid/metabolism, Amphetamines/*pharmacology, Animals, Brain research, Corpus Striatum/*metabolism, Dopamine D2, Dopamine/*metabolism, Dopamine/drug effects, Electrochemistry, Inbred Strains, Male, Pehek E A, Rats, Receptors, Sulpiride/*pharmacology, Yamamoto B K

A noninflammatory interleukin-1beta fragment stimulates fetal lung fluid absorption in guinea pigs.

We have previously demonstrated that full-length interleukin (IL)-1beta can induce and stimulate lung fluid absorption in near-term guinea pig fetuses via stimulation of fetal cortisol synthesis and release. To develop a potentially clinically useful…

A novel bile acid-activated vitamin D receptor signaling in human hepatocytes.

Vitamin D receptor (VDR) is activated by natural ligands, 1alpha,

Tags: 2010, Calcitriol/*metabolism, Calcitriol/pharmacology, Cell Membrane/drug effects/metabolism, Cell Nucleus/drug effects/metabolism, Chiang John Y L, Cholesterol 7-alpha-Hydroxylase/antagonists & inhibitors/genetics, Department of Integrative Medical Sciences, Ellis Ewa, Enzyme Activation/drug effects, Extracellular Signal-Regulated MAP Kinases/antagonists & inhibitors, Genetic/genetics, Han Shuxin, Hep G2 Cells, Hepatocyte Nuclear Factor 4/metabolism, Hepatocytes/*drug effects/enzymology/*metabolism, Humans, Intracellular Space/drug effects/metabolism, Li Tiangang, Ligands, Lithocholic Acid/*pharmacology, Mitogen-Activated Protein Kinase Kinases/metabolism, Molecular endocrinology (Baltimore, Md.), NEOMED College of Medicine, Phosphorylation/drug effects, Phosphotyrosine/metabolism, Promoter Regions, Protein Kinase Inhibitors/pharmacology, Protein Transport/drug effects, Proto-Oncogene Proteins c-raf/metabolism, Receptors, Retinoid X Receptor alpha/metabolism, Signal Transduction/*drug effects, src-Family Kinases/metabolism, Steroid Hydroxylases/genetics/metabolism, Strom Stephen, Vitamin D3 24-Hydroxylase

A novel mechanism of neurokinin-1 receptor resensitization.

Prolonged or repeated activation of many G protein-coupled receptors induces rapid desensitization followed by a period during which receptors are resensitized. In this study, concanavalin A (Con A) and monensin were used to investigate the…

Tags: 2002, Animals, Bennett V J, Cell Membrane/drug effects/metabolism, CHO Cells, Concanavalin A/pharmacology, Cricetinae, Monensin/pharmacology, Neurokinin-1/*agonists/*metabolism, Perrine S A, Phosphorylation/drug effects, Rats, Receptors, Simmons M A, The Journal of pharmacology and experimental therapeutics

A Western diet induced NAFLD in LDLR(-/)(-) mice is associated with reduced hepatic glutathione synthesis.

Oxidative stress plays a key role in the pathogenesis of non-alcoholic fatty liver disease (NAFLD). Glutathione is the major anti-oxidant involved in cellular oxidative defense, however there are currently no simple non-invasive methods for assessing…

Activation of heterotrimeric G-proteins independent of a G-protein coupled receptor and the implications for signal processing.

Heterotrimeric G-proteins are key transducers for signal transfer from outside the cell, mediating signals emanating from cell-surface G-protein coupled receptors (GPCR). Many, if not all, subtypes of heterotrimeric G-proteins are also regulated by…

Tags: *Signal Transduction, 2005, Animals, Biological, Cismowski M J, G-Protein-Coupled/*metabolism, Heterotrimeric GTP-Binding Proteins/*metabolism, Humans, Lanier S M, Models, Receptors, Reviews of physiology, biochemistry and pharmacology

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…

Activation of synaptic group II metabotropic glutamate receptors induces long-term depression at GABAergic synapses in CNS neurons.

Metabotropic glutamate receptor (mGluR)-dependent homosynaptic long-term depression (LTD) has been studied extensively at glutamatergic synapses in the CNS. However, much less is known about heterosynaptic long-term plasticity induced by mGluRs at…

Tags: 2013, Amino Acids/pharmacology, Animals, Chick Embryo, Cochlear Nucleus/drug effects/metabolism, Curry Rebecca J, Cyclopropanes/pharmacology, Department of Anatomy & Neurobiology, Dinh Emilie Hoang, Excitatory Amino Acid Agonists/pharmacology, Excitatory Amino Acid Antagonists/pharmacology, Excitatory Postsynaptic Potentials/drug effects/physiology, GABAergic Neurons/drug effects/*metabolism, Glycine/analogs & derivatives/pharmacology, Hamlet William R, Inhibitory Postsynaptic Potentials/drug effects/physiology, Liu Yu-Wei, Long-Term Synaptic Depression/drug effects/*physiology, Lu Yong, Metabotropic Glutamate/agonists/antagonists & inhibitors/*metabolism, NEOMED College of Medicine, Neural Inhibition/drug effects/physiology, Receptors, Shi Wei, Synapses/drug effects/*metabolism, Synaptic Transmission/drug effects/*physiology, Tang Zheng-Quan, The Journal of neuroscience : the official journal of the Society for Neuroscience, Xanthenes/pharmacology

Acute and subchronic effects of methylenedioxymethamphetamine [(+/-)MDMA] on locomotion and serotonin syndrome behavior in the rat.

Specific behaviors comprising the serotonin syndrome (low body posture, forepaw treading, headweaving) and the autonomic signs of piloerection and salivation were determined and analyzed with locomotor activity in response to MDMA at three doses…

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…

Aldo-keto reductase 1B7 is a target gene of FXR and regulates lipid and glucose homeostasis.

Aldo-keto reductase 1B7 (AKR1B7) is proposed to play a role in detoxification of by-products of lipid peroxidation. In this article, we show that activation of the nuclear receptor farnesoid X receptor (FXR) induces AKR1B7 expression in the liver and…

All-trans-retinoic acid ameliorates hepatic steatosis in mice by a novel transcriptional cascade.

UNLABELLED: Mice deficient in small heterodimer partner (SHP) are protected from diet-induced hepatic steatosis resulting from increased fatty acid oxidation and decreased lipogenesis. The decreased lipogenesis appears to be a direct consequence of…

Alteration of dopamine release by rat caudate putamen tissues superfused with alpha 2-macroglobulin.

Monoamine-activated alpha-2-macroglobulin (alpha 2M) has been shown to decrease the dopamine concentrations in rat caudate putamen (CP) in vivo as well as inhibit choline acetyltransferase activities in the culture of basal forebrain neurons. In this…

Ambient GABA-activated tonic inhibition sharpens auditory coincidence detection via a depolarizing shunting mechanism.

Tonic inhibition mediated by extrasynaptic GABA(A) receptors (GABA(A)Rs) has emerged as a novel form of neural inhibition in the CNS. However, little is known about its presence and function in the auditory system. Using whole-cell recordings in…

Analgesic effects of serotonin and receptor-selective serotonin agonists in the rat spinal cord.

1. Serotonin (5-HT) and selective 5-HT receptor agonists were administered intrathecally (i.t.) in rats, and the antinociceptive efficacy of these agents was assessed on the tail-flick and hot plate tests. 2. The 5-HT receptor agonists examined in…

Baclofen-induced disinhibition in area CA1 of rat hippocampus is resistant to extracellular Ba2+.

The mechanism of disinhibition produced by (+/-)-baclofen was studied using intracellular recording in area CA1 of rat hippocampal slices. Baclofen reversibly depressed monosynaptic IPSPs evoked by direct activation of interneurons in the presence of…

Tags: 1991, 2-Amino-5-phosphonovalerate/pharmacology, Animals, Baclofen/antagonists & inhibitors/*pharmacology, Barium/*pharmacology, Brain research, Drug Resistance/physiology, Evoked Potentials/drug effects, GABA-A/*drug effects, Harrison N L, Hippocampus/*drug effects, In Vitro Techniques, Interneurons/drug effects, Lambert N A, Neural Inhibition/drug effects, Quinoxalines/pharmacology, Rats, Receptors, Teyler T J

Beta-adrenoceptor stimulation of alveolar fluid clearance is increased in rats with heart failure.

The alveolar epithelium plays a critical role in resolving pulmonary edema. We thus hypothesized that its function might be upregulated in rats with heart failure, a condition that severely challenges the lung's ability to maintain fluid balance.…

Beyond thermoregulation: metabolic function of cetacean blubber in migrating bowhead and beluga whales.

The processes of lipid deposition and utilization, via the gene leptin (Lep), are poorly understood in taxa with varying degrees of adipose storage. This study examines how these systems may have adapted in marine aquatic environments inhabited by…

Bile acid metabolism and signaling.

Bile acids are important physiological agents for intestinal nutrient absorption and biliary secretion of lipids, toxic metabolites, and xenobiotics. Bile acids also are signaling molecules and metabolic regulators that activate nuclear receptors and…

Bile acid receptors in non-alcoholic fatty liver disease.

Accumulating data have shown that bile acids are important cell signaling molecules, which may activate several signaling pathways to regulate biological processes. Bile acids are endogenous ligands for the farnesoid X receptor (FXR) and TGR5, a…

Bile acid regulation of gene expression: roles of nuclear hormone receptors.

Bile acids derived from cholesterol and oxysterols derived from cholesterol and bile acid synthesis pathways are signaling molecules that regulate cholesterol homeostasis in mammals. Many nuclear receptors play pivotal roles in the regulation of bile…

Tags: 2002, Animals, Bile Acids and Salts/*physiology, Chiang John Y L, Cytoplasmic and Nuclear/*physiology, Department of Integrative Medical Sciences, Endocrine reviews, Gene Expression Regulation/*physiology, Humans, NEOMED College of Medicine, Receptors

Bile acid regulation of hepatic physiology: III. Bile acids and nuclear receptors.

Bile acids are physiological detergents that facilitate excretion, absorption, and transport of fats and sterols in the intestine and liver. Recent studies reveal that bile acids also are signaling molecules that activate several nuclear receptors…

Tags: 2003, American journal of physiology. Gastrointestinal and liver physiology, Animals, Bile Acids and Salts/biosynthesis/genetics/*physiology, Bile/*physiology, Cardiovascular Diseases/genetics/physiopathology, Chiang John Y L, Cholesterol/physiology, Cytoplasmic and Nuclear/*physiology, Department of Integrative Medical Sciences, Feedback/physiology, Gene Expression Regulation/physiology, Humans, Liver Diseases/genetics/physiopathology, Liver/*physiology, NEOMED College of Medicine, Receptors

Bile acid signaling in metabolic disease and drug therapy.

Bile acids are the end products of cholesterol catabolism. Hepatic bile acid synthesis accounts for a major fraction of daily cholesterol turnover in humans. Biliary secretion of bile acids generates bile flow and facilitates hepatobiliary secretion…

Bile acids activate fibroblast growth factor 19 signaling in human hepatocytes to inhibit cholesterol 7alpha-hydroxylase gene expression.

UNLABELLED: Mouse fibroblast growth factor 15 (FGF15) and human ortholog FGF19 have been identified as the bile acid-induced intestinal factors that mediate bile acid feedback inhibition of cholesterol 7alpha-hydroxylase gene (C YP7A1) transcription…

Tags: 2009, Butadienes/pharmacology, Carcinoma, Cell Line, Chenodeoxycholic Acid/*pharmacology, Chiang John Y L, Cholesterol 7-alpha-Hydroxylase/*biosynthesis, Cytoplasmic and Nuclear/metabolism/physiology, Department of Integrative Medical Sciences, DNA-Binding Proteins/metabolism, Fibroblast Growth Factor, Fibroblast Growth Factors/drug effects/*physiology, Gene Expression/drug effects, Hepatocellular/metabolism, Hepatocytes/metabolism, Hepatology (Baltimore, Md.), Humans, Isoxazoles/pharmacology, Li Tiangang, Mitogen-Activated Protein Kinase 1/metabolism, Mitogen-Activated Protein Kinase 3/metabolism, NEOMED College of Medicine, Nitriles/pharmacology, Owsley Erika, Receptor, Receptors, Signal Transduction/drug effects, Song Kwang-Hoon, Strom Stephen, Transcription Factors/metabolism, Tumor, Type 4/antagonists & inhibitors

Bile acids as metabolic regulators.

PURPOSE OF REVIEW: This review focuses on the latest understanding of the molecular mechanisms underlying the complex interactions between intestine and liver bile acid signaling, gut microbiota, and their impact on whole-body lipid, glucose and…

Bile acids: regulation of synthesis.

Bile acids are physiological detergents that generate bile flow and facilitate intestinal absorption and transport of lipids, nutrients, and vitamins. Bile acids also are signaling molecules and inflammatory agents that rapidly activate nuclear…

Tags: 2009, Animals, Bile Acids and Salts/*metabolism, Biological, Chiang John Y L, Cholesterol 7-alpha-Hydroxylase/metabolism, Cytoplasmic and Nuclear/metabolism, Department of Integrative Medical Sciences, Humans, Journal of lipid research, Models, NEOMED College of Medicine, Receptors, Signal Transduction/physiology

Blockade of the late IPSP in rat CA1 hippocampal neurons by 2-hydroxy-saclofen.

The effects of the GABAB receptor antagonist 2-hydroxy-saclofen were studied using intracellular recording of synaptic potential from CA1 hippocampal neurons.

Tags: 1989, Action Potentials/drug effects, Animals, Baclofen/*analogs & derivatives/pharmacology, GABA-A Receptor Antagonists, GABA-A/*physiology, Harrison N L, Hippocampus/drug effects/*physiology, In Vitro Techniques, Kerr D I, Lambert N A, Neural Inhibition/*drug effects, Neuroscience letters, Ong J, Prager R H, Rats, Receptors, Teyler T J

Calcitonin gene-related peptide-receptor component protein expression in the uterine cervix, lumbosacral spinal cord, and dorsal root ganglia.

The neuropeptide calcitonin gene-related peptide (CGRP) may play a role in neurogenic inflammation, tissue remodeling of the uterine cervix, promoting vasodilation, parturition, and processing of sensory information in the spinal cord.…

Tags: 2002, Animals, Calcitonin Gene-Related Peptide/*biosynthesis/immunology/metabolism, Cervix Uteri/*metabolism, Dickerson I M, Female, Ganglia, Lumbosacral Region, Papka R E, Peptides, Pokabla M J, Rats, Receptors, Spinal Cord/*metabolism, Spinal/*metabolism, Sprague-Dawley, Uterus/metabolism

Castration differentially alters [3H]nisoxetine binding to norepinephrine uptake sites in olfactory bulb and frontal cortex of male rats.

In the present study, [3H]nisoxetine binding to norepinephrine (NE) uptake sites and [3H]norepinephrine uptake were investigated within olfactory bulb (OB) and frontal cortex homogenates from intact and castrated male rats. Statistically significant…

Tags: *Orchiectomy, 1999, Adrenergic/drug effects/*metabolism, Animals, Boja J W, Dluzen D E, Fluoxetine/*analogs & derivatives/metabolism, Frontal Lobe/drug effects/*metabolism, Kinetics, Male, Norepinephrine/metabolism, Olfactory Bulb/drug effects/*metabolism, Rats, Receptors, Shang Y, Sprague-Dawley, Synapse (New York, N.Y.), Synaptosomes/drug effects/metabolism, Testosterone/pharmacology

Cholesterol 7alpha-hydroxylase protects the liver from inflammation and fibrosis by maintaining cholesterol homeostasis.

Cholesterol 7alpha-hydroxylase (CYP7A1) plays a critical role in control of bile acid and cholesterol homeostasis. Bile acids activate farnesoid X receptor (FXR) and Takeda G protein-coupled receptor 5 (TGR5) to regulate lipid, glucose, and energy…

Cholinergic disinhibition in area CA1 of the rat hippocampus is not mediated by receptors located on inhibitory neurons.

We studied the effects of carbamylcholine (carbachol; CCh) on monosynaptic inhibitory postsynaptic potentials (IPSPs) evoked in the presence of the excitatory amino acid receptor antagonists 6,7-dinitroquinoxaline-2,3-dione (DNQX) and…

Cholinergic neurons of the pelvic autonomic ganglia and uterus of the female rat: distribution of axons and presence of muscarinic receptors.

Acetylcholine (ACh) stimulates contraction of the uterus and dilates the uterine arterial supply. Uterine cholinergic nerves arise from the paracervical ganglia and were, in the past, characterized based on acetylcholinesterase (AChE) histochemistry.…

Comparative aspects of hippocampal and neocortical long-term potentiation.

Long-term potentiation (LTP) is a candidate for the synaptic alternations underlying memory storage in the mammalian CNS. In this chapter LTP in hippocampus and in visual neocortex are compared. Comparisons of the optimal tetanus parameters revealed…

Tags: 1989, Action Potentials, Animals, Electric Stimulation, Evoked Potentials, Hippocampus/*physiology, Journal of neuroscience methods, Memory/physiology, N-Methyl-D-Aspartate, Neurotransmitter/*physiology, Receptors, Teyler T J, Visual Cortex/*physiology

Comparison of inotropic and chronotropic effects of vasoactive intestinal peptide in isolated dog atria

The positive chronotropic and inotropic effects of vasoactive intestinal peptide, VIP, were studied in an isolated canine right atrial preparation, Atria were removed, maintained in a bath, and perfused with Tyrode's solution. Contractile force and…

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