Browse Items · NEOMED Bibliography Database

The NMDA receptor antagonist MK-801 produces ethanol-like discrimination in the rat.

Two groups of rats, one derived from N/Nih stock and the second from the (putatively) serotonin-compromised Fawn-Hooded line, were trained to discriminate ethanol from its vehicle in a drug discrimination paradigm. Once each of the two groups…

Tags: 1993, Alcohol (Fayetteville, N.Y.), Animals, Department of Anatomy & Neurobiology, Discrimination Learning/*drug effects, Dizocilpine Maleate/*pharmacology, Ethanol/*pharmacology, Gordon T L, McBurney D M, Meehan S M, N-Methyl-D-Aspartate/physiology, NEOMED College of Medicine, Rats, Receptors, Schechter M D

Icatibant for the treatment of orolingual angioedema following the administration of tissue plasminogen activator.

Tags: 2018, Airway Management, Angioedema, Angioedema – Drug Therapy, Brooks Steven, Brown Emily, Campana Christina M, Cell Surface – Antagonists and Inhibitors, Department of Emergency Medicine, Icatibant, NEOMED College of Medicine, Receptors, stroke, The American journal of emergency medicine, Tissue plasminogen activator, Tissue Plasminogen Activator – Therapeutic Use, Zimmerman Jacob

Stimulation of distal airspace fluid clearance in guinea pigs involves bumetanide-sensitive ion transport.

OBJECTIVE: This study was undertaken to test the hypothesis that beta-adrenoceptor stimulation of fetal lung fluid absorption in near-term guinea pig fetuses involves bumetanide-sensitive ion transport. STUDY DESIGN: Fetuses were obtained from…

Mutation in osteoactivin decreases bone formation in vivo and osteoblast differentiation in vitro.

We have previously identified osteoactivin (OA), encoded by Gpnmb, as an osteogenic factor that stimulates osteoblast differentiation in vitro. To elucidate the importance of OA in osteogenesis, we characterized the skeletal phenotype of a mouse…

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…

Structure-activity relationships of pentacycloundecylamines at the

Prompted by our interest in neuroprotective agents with multiple mechanisms of action, we assessed the structure-activity relationship of a series of pentacycloundecylamine derivatives previously shown to have both L-type calcium channel blocking…

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

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

Impact of circadian nuclear receptor REV-ERBalpha on midbrain dopamine production and mood regulation.

The circadian nature of mood and its dysfunction in affective disorders is well recognized, but the underlying molecular mechanisms are still unclear. Here, we show that the circadian nuclear receptor REV-ERBalpha, which is associated with bipolar…

Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists.

Farnesoid X receptor (FXR), a nuclear receptor mainly distributed in liver and intestine, has been regarded as a potential target for the treatment of various metabolic diseases, cancer and infectious diseases related to liver. Starting from two…

The role of the N-terminal and mid-region residues of substance P in regulating functional selectivity at the tachykinin NK1 receptor.

Previous studies have shown that tachykinin peptide ligands of the tachykinin NK1 receptor exhibit functional selectivity with respect to signal activation and desensitization. The differences are most dramatic between the naturally occurring…

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…

Metabotropic glutamate and GABA receptors modulate cellular excitability and glutamatergic transmission in chicken cochlear nucleus angularis neurons.

Neurons in the avian cochlear nucleus angularis (NA) receive glutamatergic input from the auditory nerve, and GABAergic input from the superior olivary nucleus. Physiologically heterogeneous, NA neurons perform multiple functions including encoding…

Leukotriene D4 and prostaglandin E2 signals synergize and potentiate vascular inflammation in a mast cell-dependent manner through cysteinyl leukotriene receptor 1 and E-prostanoid receptor 3.

BACKGROUND: Although arachidonic acid metabolites, cysteinyl leukotrienes (cys-LTs; leukotriene [LT] C4, LTD4, and LTE4), and prostaglandin (PG) E2 are generated at the site of inflammation, it is not known whether crosstalk exists between these 2…

Development and validation of an LC-MS/MS method for determination of the L-type voltage-gated calcium channel/NMDA receptor antagonist NGP1-01 in mouse serum.

NGP1-01 (8-benzylamino-8,11-oxapentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecane) is a heterocyclic cage compound with multifunctional calcium channel blocking activity that has been demonstrated to be neuroprotective in several neurodegenerative…

Regulation of bile acid synthesis: pathways, nuclear receptors, and mechanisms.

Tags: 2004, Animals, Bile Acids and Salts/*biosynthesis, Chiang John Y L, Cytoplasmic and Nuclear/*physiology, Department of Integrative Medical Sciences, Feedback, Humans, Journal of hepatology, Lipid Metabolism, NEOMED College of Medicine, Physiological, Receptors

mGluRs modulate neuronal firing in the auditory midbrain.

The mechanisms underlying sound-evoked suppression of neuronal firing in the auditory system are poorly understood. To explore these mechanisms in the inferior colliculus (IC), agonists and antagonists targeting different groups of metabotropic…

Synaptic activity-induced Ca(2+) signaling in avian cochlear nucleus magnocellularis neurons.

Neurons of the avian cochlear nucleus magnocellularis (NM) receive glutamatergic inputs from the spiral ganglion cells via the auditory nerve and feedback GABAergic inputs primarily from the superior olivary nucleus. We investigated regulation of…

Localization and function of NK(3) subtype tachykinin receptors of layer V pyramidal neurons of the guinea-pig medial prefrontal cortex.

The NK(3) subtype of tachykinin receptor has been implicated as a modulator of synaptic transmission in several brain regions, including the cerebral cortex. The localization and expression of NK(3) receptors within the brain vary from species to…

Tags: 2008, Animals, Autoradiography/methods, Dose-Response Relationship, Drug, Drug Interactions, Excitatory Amino Acid Antagonists/pharmacology, Excitatory Postsynaptic Potentials/drug effects/radiation effects, Guinea Pigs, In Vitro Techniques, Iodine Isotopes/pharmacokinetics, Male, Medd A M, Membrane Potentials/drug effects/physiology/radiation effects, Neurokinin B/analogs & derivatives/pharmacokinetics, Neurokinin-3/agonists/antagonists & inhibitors/*metabolism, Neuroscience, Patch-Clamp Techniques, Peptide Fragments/pharmacology, Prefrontal Cortex/*cytology, Protein Binding/drug effects, Pyramidal Cells/drug effects/*metabolism, Quinolines/pharmacology, Quinoxalines/pharmacology, Receptors, Simmons M A, Sobotka-Briner C D, Substance P/analogs & derivatives/pharmacology, Valine/analogs & derivatives/pharmacology

Metabotropic glutamate receptors in auditory processing.

As the major excitatory neurotransmitter used in the vertebrate brain, glutamate activates ionotropic and metabotropic glutamate receptors (mGluRs), which mediate fast and slow neuronal actions, respectively. Important modulatory roles of mGluRs have…

Tags: 2014, Animals, Auditory Pathways/anatomy & histology/physiology, Auditory Perception/*physiology, auditory processing, Department of Anatomy & Neurobiology, excitotoxicity, Humans, Lu Y, Metabotropic Glutamate/*metabolism, mGluR, NEOMED College of Medicine, neuromodulation, Neuroscience, neurotransmission, Receptors, synaptic plasticity

Intrinsic plasticity induced by group II metabotropic glutamate receptors via enhancement of high-threshold KV currents in sound localizing neurons.

Intrinsic plasticity has emerged as an important mechanism regulating neuronal excitability and output under physiological and pathological conditions. Here, we report a novel form of intrinsic plasticity. Using perforated patch clamp recordings, we…

Non-receptor activators of heterotrimeric G-protein signaling (AGS proteins).

G-protein coupled receptor (GPCR) signaling represents one of the most conserved and ubiquitous means in mammalian cells for transferring information across the plasma membrane to the intracellular environment. Heterotrimeric G-protein subunits play…

Tags: *Signal Transduction, 2006, Animals, Biological, Cismowski Mary J, G-Protein-Coupled/*metabolism, Heterotrimeric GTP-Binding Proteins/*metabolism, Humans, Models, Receptors, Seminars in cell & developmental biology

Unconventional effects of estrogen uncovered.

The nigrostriatal dopamine system shows marked gender differences that, in many cases, can be attributable to estrogen. However, the virtual absence of conventional estrogen receptors within the nigrostriatal dopamine system has made it difficult to…

Tags: 2005, Animals, Corpus Striatum/*metabolism/physiology, Dluzen Dean E, Dopamine D2/metabolism, Dopamine/*metabolism, Estrogens/*physiology, GTP-Binding Proteins/metabolism, Humans, Receptors, Signal Transduction/physiology, Substantia Nigra/*metabolism/physiology, Trends in pharmacological sciences

Epileptic-like activity induces multiple forms of plasticity in hippocampal area CA1.

Mesial temporal lobe epilepsy is a relatively common form of epilepsy that afflicts many thousands of people. It has been suggested that the development of primary and secondary foci may involve mechanisms similar to long-term potentiation (LTP). In…

Tags: *Neuronal Plasticity, 2001, Animals, Brain research, Calcium Channels, Electrophysiology, Epilepsy/chemically induced/*physiopathology, Hippocampus/*physiopathology, Ion Channels/physiology, L-Type/physiology, Long-Evans, Long-Term Potentiation/physiology, Morgan S L, N-Methyl-D-Aspartate/metabolism, Potassium Chloride, Rats, Receptors, Synapses/physiology, Teyler T J

The effects of aging on mu and delta opioid receptors in the spinal cord of Fischer-344 rats.

Previous research has demonstrated that the antinociceptive efficacy of opioids decreases with advancing age. This study utilized radioligand binding techniques to determine if this decline is due to a change in the receptor density (Bmax) and/or…

Estrogen receptors in the spinal cord, sensory ganglia, and pelvic autonomic ganglia.

Until relatively recently, most studies of the effects of estradiol in the nervous system focused on hypothalamic, limbic, and other brain centers involved in reproductive hormone output, feedback, and behaviors. Almost no studies addressed estradiol…

Tags: 2003, Animals, Autonomic/cytology/*physiology, Estrogen/*physiology, Estrogens/physiology, Female, Female/*innervation/physiology, Ganglia, Genitalia, Humans, Hypogastric Plexus/cytology/physiology, International review of cytology, Mowa C N, Neurotransmitter Agents/physiology, Papka R E, Pregnancy, Receptors, Sensory/cytology/*physiology, Spinal Cord/cytology/*physiology

GABAa receptor-mediated field potentials are enhanced in area CA1 following prenatal cocaine exposure.

Prenatal cocaine exposure results in several documented changes in neurotransmitter receptor number and structure. Increases have been reported for cortical catecholamine and indoleamine receptor number and binding affinity, in the subunit expression…

Sensory nerves and neuropeptides in uterine cervical ripening.

At the time of parturition (fetal delivery) the uterine cervix must "ripen," becoming soft, pliable, and dilated to accommodate the fetus' delivery. The fundamental processes underlying cervical ripening remain poorly understood. Knowledge that…

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

Tachykinin peptide-induced activation and desensitization of neurokinin 1 receptors.

The actions of four tachykinins on inhibition and desensitization of the

Tags: 2003, Amino Acid Sequence, Animals, Bennett V J, CHO Cells, Cricetinae, Down-Regulation/*drug effects, Electrophysiology, Ligands, Neurokinin-1/*agonists/*metabolism, Peptides, Perrine S A, Potassium/metabolism, Protein Binding, Rana catesbeiana, Receptors, Simmons M A, Tachykinins/chemistry/*pharmacology

Substance P in the uterine cervix, dorsal root ganglia and spinal cord during pregnancy and the effect of estrogen on SP synthesis.

Prior to parturition the non-pliable uterine cervix undergoes a ripening process ("softens" and dilates) to allow a timely passage of the fetus at term. The exact mechanism(s) triggering and involved in cervical ripening are unknown, though evidence…

Nisoxetine infusion into the olfactory bulb enhances the capacity for male rats to identify conspecifics.

In the present report, the norepinephrine uptake inhibitor nisoxetine as well as a cocktail of nisoxetine and the alpha-adrenergic receptor antagonist phentolamine were infused unilaterally into the olfactory bulb during microdialysis to assess their…

G protein coupling profile of mGluR6 and expression of G alpha proteins in retinal ON bipolar cells.

Metabotropic glutamate receptor 6 (mGluR6) is a group III, pertussis toxin (PTX)-sensitive G protein coupled mGluR that plays a specialized role in the retina. Retinal ON bipolar cells, which receive direct glutamatergic input from photoreceptor…

Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor.

The NK(3) subtype of tachykinin receptor is a G protein-coupled receptor that is a potential therapeutic target for several neurological diseases, including schizophrenia. In this study, we have screened compound databases for novel NK(3) receptor…

Two components of long-term potentiation induced by different patterns of afferent activation.

Long-term potentiation (LTP) of excitatory synaptic transmission could be a mechanism underlying memory. Induction of LTP requires Ca2+ influx into postsynaptic neurons through ion channels gated by NMDA (N-methyl-D-aspartate) receptors in…

Tags: 1990, 2-Amino-5-phosphonovalerate/*pharmacology, Afferent Pathways/physiology, Animals, Calcium/*physiology, Grover L M, Hippocampus/*physiology, In Vitro Techniques, Membrane Potentials, Memory/*physiology, N-Methyl-D-Aspartate/*physiology, Nature, Neuronal Plasticity, Receptors, Synaptic Transmission, Teyler T J, Time Factors

Members of the novel UBASH3/STS/TULA family of cellular regulators suppress

The UBASH3/STS/TULA family consists of two members sharing substantial homology and a similar multi-domain architecture, which includes a C-terminal histidine phosphatase domain capable of dephosphorylating phosphotyrosine-containing substrates.…

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…

Orphan nuclear receptor oestrogen-related receptor gamma (ERRgamma) plays a key role in hepatic cannabinoid receptor type 1-mediated induction of CYP7A1 gene expression.

Bile acids are primarily synthesized from cholesterol in the liver and have important roles in dietary lipid absorption and cholesterol homoeostasis. Detailed roles of the orphan nuclear receptors regulating cholesterol 7alpha-hydroxylase (CYP7A1),…

Tags: 2015, Animals, bile acid, Bile Acids and Salts/metabolism, Cannabinoid, cannabinoid receptors, CB1/agonists/genetics/*metabolism, Cells, Chiang John Y L, Choi Hueng-Sik, Cholesterol 7-alpha-Hydroxylase/*biosynthesis/genetics, cholesterol 7alpha-hydroxylase (CYP7A1), Cultured, Cytoplasmic and Nuclear/metabolism, Department of Integrative Medical Sciences, Drug Inverse Agonism, Estrogen/genetics/*metabolism, Ethanol/pharmacology, Gene Expression, Genetic, Glycerides/pharmacology, GSK5182, HEK293 Cells, Hepatocytes/metabolism, Humans, Inbred C57BL, Jeong Won-Il, Kim Don-Kyu, Kim Seong Heon, Knockout, Lee Chul-Ho, Lee In-Kyu, Lee Ji-Min, Liver/*metabolism, Mice, NEOMED College of Medicine, oestrogen-related receptor gamma (ERRgamma), orphan nuclear receptor, Park Seung Bum, Promoter Regions, Rats, Receptor, Receptors, small heterodimer partner (SHP), Sprague-Dawley, The Biochemical journal, Transcription, Zhang Yaochen

Transcriptional regulation of the human sterol 12alpha-hydroxylase gene (CYP8B1): roles of heaptocyte nuclear factor 4alpha in mediating bile acid repression.

Sterol 12alpha-hydroxylase catalyzes the synthesis of cholic acid and controls the ratio of cholic acid over chenodeoxycholic acid in the bile. Transcription of CYP8B1 is inhibited by bile acids, cholesterol, and insulin. To study the mechanism of…

Browse Items (215 total)