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Pharmacology and physiology

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https://www.readbyqxmd.com/read/28723415/pharmacology-of-human-trace-amine-associated-receptors-therapeutic-opportunities-and-challenges
#1
REVIEW
Mark D Berry, Raul R Gainetdinov, Marius C Hoener, Mohammed Shahid
The discovery in 2001 of a G protein-coupled receptor family, subsequently termed trace amine-associated receptors (TAAR), triggered a resurgence of interest in so-called trace amines. Initial optimism quickly faded, however, as the TAAR family presented a series of challenges preventing the use of standard medicinal chemistry and pharmacology technologies. Consequently the development of basic tools for probing TAAR and translating findings from model systems to humans has been problematic. Despite these challenges the last 5 years have seen considerable advances, in particular with respect to TAAR1, which appears to function as an endogenous rheostat, maintaining central neurotransmission within defined physiological limits, in part through receptor heterodimerization yielding biased signaling outputs...
July 16, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28722758/asthma-in-the-elderly-and-late-onset-adult-asthma
#2
REVIEW
Ryan M Dunn, Paula J Busse, Michael E Wechsler
Elderly asthmatics are at a higher risk for morbidity and mortality from their asthma than younger patients. There are important age-related physiologic and immunologic changes that complicate the presentation, diagnosis and management of asthma in the aged population. Evidence suggests that elderly asthmatics are more likely to be under-diagnosed and under-treated. Additionally, elderly patients with asthma have highest rates of morbidity and mortality from their disease than younger patients. The underlying airway inflammation of asthma in this age group likely differs from younger patients and is felt to be non-Type 2 mediated...
July 19, 2017: Allergy
https://www.readbyqxmd.com/read/28722242/therapeutic-application-of-gpr119-ligands-in-metabolic-disorders
#3
REVIEW
Jin Won Yang, Hyo Seon Kim, Yong-Won Choi, Young-Mi Kim, Keon Wook Kang
GPR119 belongs to the G protein-coupled receptor family, and exhibits dual modes of action upon ligand-dependent activation: pancreatic secretion of insulin in a glucose-dependent manner, and intestinal secretion of incretins. Hence, GPR119 has emerged as a promising target for treating type 2 diabetes mellitus without causing hypoglycemia. However, despite continuous efforts by many major pharmaceutical companies, no synthetic GPR119 ligand has been approved as a new class of anti-diabetic agents thus far, nor has one passed beyond phase II clinical studies...
July 18, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28721821/current-perspectives-for-the-use-of-gonane-progesteronergic-drugs-in-the-treatment-of-central-hypoventilation-syndromes
#4
Camille Loiseau, Florence Cayetanot, Fanny Joubert, Anne-Sophie Perrin-Terrin, Philippe Cardot, Marie-Noëlle Fiamma, Alain Frugiere, Christian Straus, Laurence Bodineau
BACKGROUND: Central alveolar hypoventilation syndromes (CHS) encompass neurorespiratory diseases resulting from congenital or acquired neurological disorders. Hypercapnia, acidosis, and hypoxemia resulting from CHS negatively affect physiological functions and can be life-threatening. To date, the absence of pharmacological treatment implies that the patients must receive assisted ventilation throughout their lives. OBJECTIVE: To highlight the relevance of determining conditions in which using gonane synthetic progestins could be of potential clinical interest for the treatment of CHS...
July 19, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28721811/moving-to-the-rhythm-with-clock-circadian-genes-autophagy-mtor-and-sirt1-in-degenerative-disease-and-cancer
#5
Kenneth Maiese
BACKGROUND: The mammalian circadian clock and its associated clock genes are increasingly be recognized as critical components for a number of physiological and disease processes that extend beyond hormone release, thermal regulation, and sleep-wake cycles. New evidence suggests that clinical behavior disruptions that involve prolonged shift work and even space travel may negatively impact circadian rhythm and lead to multi-system disease. METHODS: In light of the significant role circadian rhythm can hold over the body's normal physiology as well as disease processes, we examined and discussed the impact circadian rhythm and clock genes hold over lifespan, neurodegenerative disorders, and tumorigenesis...
July 17, 2017: Current Neurovascular Research
https://www.readbyqxmd.com/read/28720875/ruthenium-conjugated-chrysin-analogues-modulate-platelet-activity-thrombus-formation-and-haemostasis-with-enhanced-efficacy
#6
Divyashree Ravishankar, Maryam Salamah, Alda Attina, Radhika Pothi, Thomas M Vallance, Muhammad Javed, Harry F Williams, Eman M S Alzahrani, Elena Kabova, Rajendran Vaiyapuri, Kenneth Shankland, Jonathan Gibbins, Katja Strohfeldt, Francesca Greco, Helen M I Osborn, Sakthivel Vaiyapuri
The constant increase in cardiovascular disease rate coupled with significant drawbacks of existing therapies emphasise the necessity to improve therapeutic strategies. Natural flavonoids exert innumerable pharmacological effects in humans. Here, we demonstrate the effects of chrysin, a natural flavonoid found largely in honey and passionflower on the modulation of platelet function, haemostasis and thrombosis. Chrysin displayed significant inhibitory effects on isolated platelets, however, its activity was substantially reduced under physiological conditions...
July 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28716904/intracellular-zinc-activates-kcnq-channels-by-reducing-their-dependence-on-phosphatidylinositol-4-5-bisphosphate
#7
Haixia Gao, Aurélien Boillat, Dongyang Huang, Ce Liang, Chris Peers, Nikita Gamper
M-type (Kv7, KCNQ) potassium channels are proteins that control the excitability of neurons and muscle cells. Many physiological and pathological mechanisms of excitation operate via the suppression of M channel activity or expression. Conversely, pharmacological augmentation of M channel activity is a recognized strategy for the treatment of hyperexcitability disorders such as pain and epilepsy. However, physiological mechanisms resulting in M channel potentiation are rare. Here we report that intracellular free zinc directly and reversibly augments the activity of recombinant and native M channels...
July 17, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28714894/carbonic-anhydrase-from-porphyromonas-gingivalis-as-a-drug-target
#8
REVIEW
Claudiu T Supuran, Clemente Capasso
Periodontitis originates from a microbial synergy causing the development of a mouth microbial imbalance (dysbiosis), consisting of a microbial community composed of anaerobic bacteria. Most studies concerning the treatment of periodontitis have primarily take into account the Gram-negative bacterium Porphyromonas gingivalis, because it is a prominent component of the oral microbiome and a successful colonizer of the oral epithelium. Here, we focus our attention on the study of the carbonic anhydrases (CAs, EC 4...
July 15, 2017: Pathogens
https://www.readbyqxmd.com/read/28714737/breastfeeding-a-review-of-its-physiology-and-galactogogue-plants-in-view-of-traditional-persian-medicine
#9
Roghayeh Javan, Behjat Javadi, Zohre Feyzabadi
INTRODUCTION: The beneficial effects of breastfeeding for the infant and mother are well recognized. Many natural products are reputed to be galactogogue agents in major Traditional Persian Medicine (TPM) textbooks. The aim of this study is to review those medicinal plants that are reported to be effective in increasing breast milk in TPM and to compare the data from TPM texts with the findings of modern pharmacological and clinical research. MATERIALS AND METHODS: Data on the medicinal plants used to increase breast milk were obtained from major TPM textbooks...
July 17, 2017: Breastfeeding Medicine: the Official Journal of the Academy of Breastfeeding Medicine
https://www.readbyqxmd.com/read/28714404/current-and-emerging-strategies-in-osteoporosis-management
#10
Stefka Ivanova, Liliya Vasileva
The abnormal loss of bone tissue is defined as osteoporosis. Increased risk of fractures, low bone mineral density (BMD) and loss of the structural and biomechanical properties of the bone tissue characterize this pathological condition. Physiologically bone undergoes a continuous remodeling process involving balance between the activity of osteoblast and osteoclast. Disruption in this balanced condition increases the risk of osteoporosis. Both sexes are affected, but with higher prevalence in women after menopause...
July 14, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28713881/drug-delivery-and-nanoformulations-for-the-cardiovascular-system
#11
W J Geldenhuys, M T Khayat, J Yun, M A Nayeem
Therapeutic delivery to the cardiovascular system may play an important role in the successful treatment of a variety of disease state, including atherosclerosis, ischemic-reperfusion injury and other types of microvascular diseases including hypertension. In this review we evaluate the different options available for the development of suitable delivery systems that include the delivery of small organic compounds [adenosin A2A receptor agonist (CGS 21680), CYP-epoxygenases inhibitor (N-(methylsulfonyl)-2-(2-propynyloxy)-benzenehexanamide, trans-4-[4-(3-adamantan-1-ylureido)cyclohexyloxy] benzoic acid), soluble epoxide hydrolase inhibitor (N-methylsulfonyl-12,12-dibromododec-11-enamide), PPARγ agonist (rosiglitazone) and PPARγ antagonist (T0070907)], nanoparticles, peptides, and siRNA to the cardiovascular system...
February 2017: Res Rev Drug Deliv
https://www.readbyqxmd.com/read/28713569/kctd12-modulation-of-gaba-b-receptor-function
#12
Melody Li, Carol J Milligan, Haiyan Wang, Andrew Walker, Leonid Churilov, Andrew J Lawrence, Christopher A Reid, Seth C Hopkins, Steven Petrou
The molecular composition and functional diversity of native GABAB receptors (GABABR) are still poorly understood, thus hindering development of selective GABABR ligands. Potassium channel tetramerization domain-containing protein (KCTD) 12 is a GABABR auxiliary subunit and mouse KCTD12 can alter GABABR function. In this study, we sought to characterize the effects of human KCTD12 on GABABR kinetics and pharmacology, using an automated electrophysiological assay. Seizure susceptibility and ethanol consumption were also investigated in a KCTD12 knockout mouse model...
August 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28713258/relationship-of-topology-multiscale-phase-synchronization-and-state-transitions-in-human-brain-networks
#13
Minkyung Kim, Seunghwan Kim, George A Mashour, UnCheol Lee
How the brain reconstitutes consciousness and cognition after a major perturbation like general anesthesia is an important question with significant neuroscientific and clinical implications. Recent empirical studies in animals and humans suggest that the recovery of consciousness after anesthesia is not random but ordered. Emergence patterns have been classified as progressive and abrupt transitions from anesthesia to consciousness, with associated differences in duration and electroencephalogram (EEG) properties...
2017: Frontiers in Computational Neuroscience
https://www.readbyqxmd.com/read/28713161/functional-expression-of-the-ca-2-signaling-machinery-in-human-embryonic-stem-cells
#14
Ji-Jun Huang, Yi-Jie Wang, Min Zhang, Peng Zhang, He Liang, Hua-Jun Bai, Xiu-Jian Yu, Huang-Tian Yang
Emerging evidence suggests that Ca(2+) signals are important for the self-renewal and differentiation of human embryonic stem cells (hESCs). However, little is known about the physiological and pharmacological properties of the Ca(2+)-handling machinery in hESCs. In this study we used RT-PCR and Western blotting to analyze the expression profiles of genes encoding Ca(2+)-handling proteins; we also used confocal Ca(2+) imaging and pharmacological approaches to determine the contribution of the Ca(2+)-handling machinery to the regulation of Ca(2+) signaling in hESCs...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28711908/the-2-aminoethoxydiphenyl-borate-analog-dpb161-blocks-store-operated-ca2-entry-in-acutely-dissociated-rat-submandibular-cells
#15
Kunkun Xia, Zegang Ma, Jianxin Shen, Menghan Li, Baoke Hou, Ming Gao, Shuijun Zhang, Jie Wu
Cellular Ca2+ signals play a critical role in cell physiology and pathology. In most non-excitable cells, store-operated Ca2+ entry (SOCE) is an important mechanism by which intracellular Ca2+ signaling is regulated. However, few drugs can selectively modulate SOCE. 2-Aminoethoxydiphenyl borate (2APB) and its analogs (DPB162 and DPB163) have been reported to inhibit SOCE. Here, we examined the effects of another 2-APB analog, DPB161 on SOCE in acutely-isolated rat submandibular cells. Both patch-clamp recordings and Ca2+ imaging showed that upon removal of extracellular Ca2+ ([Ca2+]o=0), rat submandibular cells were unable to maintain ACh-induced Ca2+ oscillations, but restoration of [Ca2+]o to refill Ca2+ stores enable recovery of these Ca2+ oscillations...
June 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/28710553/metabolism-and-distribution-of-pharmacological-homoarginine-in-plasma-and-main-organs-of-the-anesthetized-rat
#16
Duygu Naile Günes, Arslan Arinc Kayacelebi, Erik Hanff, Joel Lundgren, Björn Redfors, Dimitrios Tsikas
L-Homoarginine (hArg) and guanidinoacetate (GAA) are produced from L-arginine (Arg) by the catalytic action of arginine:glycine amidinotransferase. Guanidinoacetate methyltransferase methylates GAA on its non-guanidine N atom to produce creatine. Arg and hArg are converted by nitric oxide synthase (NOS) to nitric oxide (NO). NO is oxidized to nitrite and nitrate which circulate in the blood and are excreted in the urine. Asymmetric dimethylarginine (ADMA), an NOS inhibitor, is widely accepted to be exclusively produced after asymmetric N (G)-methylation of Arg residues in proteins and their regular proteolysis...
July 14, 2017: Amino Acids
https://www.readbyqxmd.com/read/28710078/endocrinology-and-the-brain-corticotropin-releasing-hormone-signaling
#17
Carolina Inda, Natalia G Armando, Paula A Dos Santos Claro, Susana Silberstein
Corticotropin-releasing hormone (CRH) is a key player of basal and stress activated responses in the hypothalamic-pituitary-adrenal axis (HPA) and in extrahypothalamic circuits, where it functions as a neuromodulator to orchestrate humoral and behavioral adaptive responses to stress. This review describes molecular components and cellular mechanisms involved in CRH signaling downstream of its G protein-coupled receptors (GPCRs) CRHR1 and CRHR2, and summarizes recent findings that challenge the classical view of GPCR signaling, and impact on our understanding of CRHRs function...
July 14, 2017: Endocrine Connections
https://www.readbyqxmd.com/read/28709786/-pcsk-9-inhibitors-effects-on-ldl-c-and-future-implications-what-you-should-know
#18
P Corral, A J Ruiz
The discovery of proprotein convertase subtilisin/kexin type 9 (PCSK9) in 2003 in families with familial hypercholesterolemia (HF) later generated the development of pharmacological strategies in order to inhibit this protein. Twelve years after this discovery, the first two biological compounds (monoclonal antibodies) were approved, which have been shown to substantially decrease LDL-C and other lipid subfractions. The objective of the present article is to review the history of the discovery of PCSK9, its physiology and pathophysiology and subsequent pharmacological development...
July 11, 2017: Hipertensión y Riesgo Vascular
https://www.readbyqxmd.com/read/28709449/a-novel-alzheimer-s-disease-drug-candidate-targeting-inflammation-and-fatty-acid-metabolism
#19
Daniel Daugherty, Joshua Goldberg, Wolfgang Fischer, Richard Dargusch, Pamela Maher, David Schubert
BACKGROUND: CAD-31 is an Alzheimer's disease (AD) drug candidate that was selected on the basis of its ability to stimulate the replication of human embryonic stem cell-derived neural precursor cells as well as in APPswe/PS1ΔE9 AD mice. To move CAD-31 toward the clinic, experiments were undertaken to determine its neuroprotective and pharmacological properties, as well as to assay its therapeutic efficacy in a rigorous mouse model of AD. RESULTS: CAD-31 has potent neuroprotective properties in six distinct nerve cell assays that mimic toxicities observed in the old brain...
July 14, 2017: Alzheimer's Research & Therapy
https://www.readbyqxmd.com/read/28707455/human-brown-adipose-tissue-as-a-target-for-obesity-management-beyond-cold-induced-thermogenesis
#20
REVIEW
R K C Loh, B A Kingwell, A L Carey
Elevating energy expenditure via adaptive thermogenesis in brown adipose tissue (BAT) is a potential strategy to reverse obesity. Much early enthusiasm for this approach, based on rodent studies, was tempered by the belief that BAT was relatively inconsequential in healthy adult humans. Interest was reinvigorated a decade ago when a series of studies re-identified BAT, primarily in upper thoracic regions, in adults. Despite the ensuing explosion of pre-clinical investigations and identification of an extensive list of potential target molecules for BAT recruitment, our understanding of human BAT physiology remains limited, particularly regarding interventions which might hold therapeutic promise...
July 14, 2017: Obesity Reviews: An Official Journal of the International Association for the Study of Obesity
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