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Pharmacology and physiology

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https://www.readbyqxmd.com/read/28930537/differences-in-ion-channel-phenotype-and-function-between-humans-and-animal-models
#1
Mark R Tanner, Christine Beeton
Ion channels play crucial roles in regulating a broad range of physiological processes. They form a very large family of transmembrane proteins. Their diversity results from not only a large number of different genes encoding for ion channel subunits but also the ability of subunits to assemble into homo- or heteromultimers, the existence of splice variants, and the expression of different regulatory subunits. These characteristics and the existence of very selective modulators make ion channels very attractive targets for therapy in a wide variety of pathologies...
January 1, 2018: Frontiers in Bioscience (Landmark Edition)
https://www.readbyqxmd.com/read/28930139/critical-analysis-on-characterization-systemic-effect-and-therapeutic-potential-of-beta-sitosterol-a-plant-derived-orphan-phytosterol
#2
REVIEW
Muhammad Shahdaat Bin Sayeed, Selim Muhammad Rezaul Karim, Tasnuva Sharmin, Mohammed Monzur Morshed
Beta-sitosterol (BS) is a phytosterol, widely distributed throughout the plant kingdom and known to be involved in the stabilization of cell membranes. To compile the sources, physical and chemical properties, spectral and chromatographic analytical methods, synthesis, systemic effects, pharmacokinetics, therapeutic potentials, toxicity, drug delivery and finally, to suggest future research with BS, classical as well as on-line literature were studied. Classical literature includes classical books on ethnomedicine and phytochemistry, and the electronic search included Pubmed, SciFinder, Scopus, the Web of Science, Google Scholar, and others...
November 15, 2016: Medicines (Basel, Switzerland)
https://www.readbyqxmd.com/read/28929349/depression-and-anxiety-in-polycystic-ovary-syndrome-etiology-and-treatment
#3
REVIEW
Laura G Cooney, Anuja Dokras
PURPOSE OF REVIEW: Polycystic ovary syndrome (PCOS) is the most common endocrine disorder in reproductive age women and is associated with an increased prevalence of depression and anxiety symptoms. This review presents potential mechanisms for this increased risk and outlines treatment options. RECENT FINDINGS: Women with PCOS have increased odds of depressive symptoms (OR 3.78; 95% CI 3.03-4.72) and anxiety symptoms (OR 5.62; 95% CI 3.22-9.80). Obesity, insulin resistance, and elevated androgens may partly contribute to this association...
September 20, 2017: Current Psychiatry Reports
https://www.readbyqxmd.com/read/28928637/alpha7-nicotinic-acetylcholine-receptors-play-a-predominant-role-in-the-cholinergic-potentiation-of-n-methyl-d-aspartate-evoked-firing-responses-of-hippocampal-ca1-pyramidal-cells
#4
Zsolt K Bali, Lili V Nagy, István Hernádi
The aim of the present study was to identify in vivo electrophysiological correlates of the interaction between cholinergic and glutamatergic neurotransmission underlying memory. Extracellular spike recordings were performed in the hippocampal CA1 region of anesthetized rats in combination with local microiontophoretic administration of N-methyl-D-aspartate (NMDA) and acetylcholine (ACh). Both NMDA and ACh increased the firing rate of the neurons. Furthermore, the simultaneous delivery of NMDA and ACh resulted in a more pronounced excitatory effect that was superadditive over the sum of the two mono-treatment effects and that was explained by cholinergic potentiation of glutamatergic neurotransmission...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28927993/voltage-gated-sodium-channel-%C3%AE-subunits-the-power-outside-the-pore-in-brain-development-and-disease
#5
REVIEW
Jacob M Hull, Lori L Isom
Voltage gated sodium channels (VGSCs) were first identified in terms of their role in the upstroke of the action potential. The underlying proteins were later identified as saxitoxin and scorpion toxin receptors consisting of α and β subunits. We now know that VGSCs are heterotrimeric complexes consisting of a single pore forming α subunit joined by two β subunits; a noncovalently linked β1 or β3 and a covalently linked β2 or β4 subunit. VGSC α subunits contain all the machinery necessary for channel cell surface expression, ion conduction, voltage sensing, gating, and inactivation, in one central, polytopic, transmembrane protein...
September 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28927115/wee1-inhibition-by-mk1775-as-a-single-agent-therapy-inhibits-ovarian-cancer-viability
#6
Minghui Zhang, Donye Dominguez, Siqi Chen, Jie Fan, Lei Qin, Alan Long, Xia Li, Yi Zhang, Huirong Shi, Bin Zhang
Wee1-like protein kinase (WEE1) physiologically serves a key function in maintaining the integrity of the cell genome through mediating the activation of cyclin-dependent kinase (CDK)1 and CDK2. Increased expression of WEE1 has been associated with the poor prognosis of patients with ovarian cancer. The present study aimed at examining the in vitro and in vivo antitumor activity of MK1775, a potent pharmacological inhibitor of WEE1, as a single agent against ovarian cancer cells. The cytotoxicity of MK1775 was examined in a panel of tumor cells using MTT in vitro...
September 2017: Oncology Letters
https://www.readbyqxmd.com/read/28925940/zebrafish-as-a-model-for-the-study-of-microvascular-complications-of-diabetes-and-their-mechanisms
#7
REVIEW
Karl Heckler, Jens Kroll
Diabetes mellitus (DM) is a crucial metabolic disease that leads to severe disorders. These include macrovascular complications such as myocardial infarction, stroke, and peripheral artery disease and microvascular complications including diabetic nephropathy, neuropathy, and retinopathy. Diabetes mellitus, along with its associated organ pathologies, is one of the key problems in today's medicine. Zebrafish is an upcoming disease model organism in diabetes research. Its glucose metabolism and the pathways of reactive metabolite formation are very similar to those of humans...
September 19, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28923174/27-hydroxycholesterol-an-endogenous-selective-estrogen-receptor-modulator
#8
REVIEW
Sisi He, Erik R Nelson
Estrogen receptors (ERs) mediate the actions of the steroidal estrogens, and are important for the regulation of several physiological and pathophysiological processes, including reproduction, bone physiology, cardiovascular physiology and breast cancer. The unique pharmacology of the ERs allows for certain ligands, such as tamoxifen, to elicit tissue- and context-specific responses, ligands now referred to as selective estrogen receptor modulators (SERMs). Recently, the cholesterol metabolite 27-hydroxychoelsterol (27HC) has been defined as an endogenous SERM, with activities in atherosclerosis, osteoporosis, breast and prostate cancers, and neural degenerative diseases...
October 2017: Maturitas
https://www.readbyqxmd.com/read/28922661/lysophosphatidic-acid-inhibits-insulin-signaling-in-primary-rat-hepatocytes-via-the-lpa3-receptor-subtype-and-is-increased-in-obesity
#9
Susann Fayyaz, Lukasz Japtok, Fabian Schumacher, Dominik Wigger, Tim Julius Schulz, Kathrin Haubold, Erich Gulbins, Heinz Völler, Burkhard Kleuser
BACKGROUND/AIMS: Obesity is a main risk factor for the development of hepatic insulin resistance and it is accompanied by adipocyte hypertrophy and an elevated expression of different adipokines such as autotaxin (ATX). ATX converts lysophosphatidylcholine to lysophosphatidic acid (LPA) and acts as the main producer of extracellular LPA. This bioactive lipid regulates a broad range of physiological and pathological responses by activation of LPA receptors (LPA1-6). METHODS: The activation of phosphatidylinositide 3-kinases (PI3K) signaling (Akt and GSK-3ß) was analyzed via western blotting in primary rat hepatocytes...
September 1, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28921641/pharmacokinetic-guided-dosing-of-new-oral-cancer-agents
#10
Catherine J Lucas, Jennifer H Martin
Generally, licensed drug-dosing recommendations for chemotherapy are based on results from clinical trials in which subjects are usually of relatively normal body size, middle-aged, and are relatively racially homogeneous, with minimal comorbidity and specific tumor characteristics. Very few nontrial patients meet these characteristics, resulting in clinical practice having to extrapolate dosing recommendations to the specific patient. There is insufficient research on the impact of obesity-associated physiological changes prevalent in patients with common cancers on standard pharmacokinetic and pharmacodynamic parameters...
October 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28921447/structure-pharmacology-and-roles-in-physiology-of-the-p2y12-receptor
#11
Ivar von Kügelgen
P2Y receptors are G-protein-coupled receptors (GPCRs) for extracellular nucleotides. The platelet ADP-receptor which has been denominated P2Y12 receptor is an important target in pharmacotherapy. The receptor couples to Gαi2 mediating an inhibition of cyclic AMP accumulation and additional downstream events including the activation of phosphatidylinositol-3-kinase and Rap1b proteins. The nucleoside analogue ticagrelor and active metabolites of the thienopyridine compounds ticlopidine, clopidogrel and prasugrel block P2Y12 receptors and, thereby, inhibit ADP-induced platelet aggregation...
September 12, 2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28921125/exogenous-cannabinoid-efficacy-merely-a-pharmacokinetic-interaction
#12
Jennifer H Martin, Jennifer Schneider, Catherine J Lucas, Peter Galettis
Endocannabinoid pharmacology is now relatively well understood with a number of endocannabinoids and endogenous cannabinoid neurotransmitters identified and the pharmacokinetics relatively well ascertained. Further, the cannabinoid receptors are now molecularly and pharmacologically characterised and the cell processes involved in endocannabinoid transcription, synthesis, post-translational modification and protein expression are reported. Endogenous cannabinoids have been shown to have key roles in immune and pain pathways and neuro-behavioural signalling including appetite regulation...
September 18, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28920044/effect-of-multisensory-stimulation-on-pain-of-eye-examination-in-preterm-infants
#13
Hossein Zeraati, Javad Shahinfar, Hamidreza Behnam Vashani, Tayebeh Reyhani
BACKGROUND: Eye examination as one of the painful procedures for retinopathy of prematurity screening can cause some pain-related physiological and behavioral changes in preterm infants. Multisensory stimulation is an analgesic non-pharmacological method that has analgesic effects on infants during painful procedures. OBJECTIVES: This study aimed to determine the effect of multisensory stimulation on induced pain during eye examination for retinopathy of prematurity screening in preterm infants...
February 2017: Anesthesiology and Pain Medicine
https://www.readbyqxmd.com/read/28919335/the-effect-of-resistance-exercise-on-sleep-a-systematic-review-of-randomized-controlled-trials
#14
REVIEW
Ana Kovacevic, Yorgi Mavros, Jennifer J Heisz, Maria A Fiatarone Singh
Impaired sleep quality and quantity are associated with future morbidity and mortality. Exercise may be an effective non-pharmacological intervention to improve sleep, however, little is known on the effect of resistance exercise. Thus, we performed a systematic review of the literature to determine the acute and chronic effects of resistance exercise on sleep quantity and quality. Thirteen studies were included. Chronic resistance exercise improves all aspects of sleep, with the greatest benefit for sleep quality...
July 19, 2017: Sleep Medicine Reviews
https://www.readbyqxmd.com/read/28918826/islamic-medicine-in-the-middle-ages
#15
EDITORIAL
Hawa Edriss, Brittany N Rosales, Connie Nugent, Christian Conrad, Kenneth Nugent
The Islamic culture flourished between the 9th and 13th centuries. Scholars from this era made significant contributions in mathematics, science and medicine. Caliphs and physicians built hospitals that provided universal care and the foundation for medical education. Physician-scientists made significant advances in medical care, surgery and pharmacology. Notable authorities include al-Razi (865-925 CE) who wrote the Kitab al-Hawi fi al-tibb (The Comprehensive Book on Medicine), a 23-volume textbook that provided the main medical curriculum for European schools into the 14th century...
September 2017: American Journal of the Medical Sciences
https://www.readbyqxmd.com/read/28917330/-oral-administration-of-medicines-in-elderly-patients-and-adaptation-of-galenic-forms
#16
Éric Pautas, Lasamy Bui, Alexandra Monti, Sébastien Krypciak, Anastasia Obraztsova, Eléna Paillaud
Physiological ageing and pathologies can have an influence on the pharmacology of numerous medicines, leading to serious iatrogenic accidents, polypharmacy and incorrect use of a medicine in elderly people. An observational study carried out in a short-stay geriatric unit focused on the issues surrounding the difficulties the elderly may encounter when taking medicines and the prevalence of the manipulation of galenic forms.
September 2017: Soins. Gérontologie
https://www.readbyqxmd.com/read/28916758/role-of-the-venus-kinase-receptor-in-the-female-reproductive-physiology-of-the-desert-locust-schistocerca-gregaria
#17
Cynthia Lenaerts, Jolien Palmans, Elisabeth Marchal, Rik Verdonck, Jozef Vanden Broeck
Venus kinase receptors (VKR) are a subfamily of invertebrate receptor tyrosine kinases, which have only recently been discovered. They contain an intracellular tyrosine kinase domain and an extracellular Venus FlyTrap domain. VKRs have been functionally and pharmacologically characterized in only two invertebrate species, namely the human parasite Schistosoma mansoni and the mosquito Aedes aegypti, where they play a crucial role in oogenesis. Here, we report the characterization of a VKR in the desert locust, Schistocerca gregaria...
September 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28916638/pharmacological-and-physiological-assessment-of-serotonin-formation-and-degradation-in-isolated-preparations-from-mouse-and-human-heart
#18
Ulrich Gergs, Franziska Jung, Igor B Buchwalow, Britt Hofmann, Andreas Simm, Hendrik Treede, Joachim Neumann
Using transgenic mice (TG) that overexpress the human 5-HT4a-receptor specifically in cardiomyocytes, we wanted to know whether 5-HT can be formed and degraded in the mammalian heart and whether this can likewise lead to inotropic and chronotropic effects in this TG model. We noted that the 5-HT precursor, 5-hydroxy-tryptophan (5-HTP), can exert inotropic and chronotropic effects in cardiac preparations from TG but not from wild type (WT): similar results were found in human atrial preparations, as well as in intact TG animals using echocardiography...
September 15, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/28915330/impact-of-adrenal-steroids-on-regulation-of-adipose-tissue
#19
Marco Infante, Andrea Armani, Caterina Mammi, Andrea Fabbri, Massimiliano Caprio
Corticosteroids are secreted by the adrenal glands and control the functions of adipose tissue via the activation of mineralocorticoid receptor (MR) and glucocorticoid receptor (GR). In turn, adipocytes release a large variety of adipokines into the bloodstream, regulating the function of several organs and tissues, including the adrenal glands, hereby controlling corticosteroid production. In adipose tissue, the activation of the MR by glucocorticoids (GC) and aldosterone affects important processes such as adipocyte differentiation, oxidative stress, autophagic flux, adipokine expression as well as local production of GC through upregulation of the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)...
September 12, 2017: Comprehensive Physiology
https://www.readbyqxmd.com/read/28915325/brown-and-beige-adipose-tissues-in-health-and-disease
#20
Liangyou Rui
Brown and beige adipocytes arise from distinct developmental origins. Brown adipose tissue (BAT) develops embryonically from precursors that also give to skeletal muscle. Beige fat develops postnatally and is highly inducible. Beige fat recruitment is mediated by multiple mechanisms, including de novo beige adipogenesis and white-to-brown adipocyte transdifferentiaiton. Beige precursors reside around vasculatures, and proliferate and differentiate into beige adipocytes. PDGFRα+Ebf2+ precursors are restricted to beige lineage cells, while another PDGFRα+ subset gives rise to beige adipocytes, white adipocytes, or fibrogenic cells...
September 12, 2017: Comprehensive Physiology
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