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cyclic Adenosine monophosphate

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https://www.readbyqxmd.com/read/28212204/1-2-4-dibromophenyl-3-6-6-trimethyl-1-5-6-7-tetrahydro-4h-indazol-4-one-a-novel-opioid-receptor-agonist-with-less-accompanying-gastrointestinal-dysfunction-than-morphine
#1
Po-Kuan Chao, Shau-Hua Ueng, Li-Chin Ou, Teng-Kuang Yeh, Wan-Ting Chang, Hsiao-Fu Chang, Shu-Chun Chen, Pao-Luh Tao, Ping-Yee Law, Horace H Loh, Ming-Fu Cheng, Jian-Ying Chuang, Chiung-Tong Chen, Chuan Shih, Shiu-Hwa Yeh
BACKGROUND: The authors investigated the pharmacology and signaling pathways of the opioid receptors modulated by compound 1, 1-(2,4-dibromophenyl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one. METHODS: In vitro studies of compound 1 were assessed by using a radioligand-binding assay (n = 3), a cyclic adenosine monophosphate assay (n = 3), a β-arrestin assay (n = 3), an internalization assay (n = 3), and an immunohistochemistry (n = 8). In vivo studies of compound 1 were characterized using a tail-flick test (n = 5 to 6), tail-clip test (n = 7), von Frey hair test (n = 5), and charcoal meal test (n = 5)...
February 17, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28211580/inhibition-of-pde5a1-guanosine-cyclic-monophosphate-cgmp-hydrolysing-activity-by-sildenafil-analogues-that-inhibit-cellular-cgmp-efflux
#2
Anna Subbotina, Aina W Ravna, Roy A Lysaa, Ruben Abagyan, Ryszard Bugno, Georg Sager
OBJECTIVES: To determine the ability of 11 sildenafil analogues to discriminate between cyclic nucleotide phosphodiesterases (cnPDEs) and to characterise their inhibitory potencies (Ki values) of PDE5A1-dependent guanosine cyclic monophosphate (cGMP) hydrolysis. METHODS: Sildenafil analogues were identified by virtual ligand screening (VLS) and screened for their ability to inhibit adenosine cyclic monophosphate (cAMP) hydrolysis by PDE1A1, PDE1B1, PDE2A1, PDE3A, PDE10A1 and PDE10A2, and cGMP hydrolysis by PDE5A, PDE6C, PDE9A2 for a low (1 nm) and high concentration (10 μm)...
February 17, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28209726/therapeutic-targeting-of-the-pathological-triad-of-extrasynaptic-nmda-receptor-signaling-in-neurodegenerations
#3
REVIEW
Hilmar Bading
Activation of extrasynaptic N-methyl-d-aspartate (NMDA) receptors causes neurodegeneration and cell death. The disease mechanism involves a pathological triad consisting of mitochondrial dysfunction, loss of integrity of neuronal structures and connectivity, and disruption of excitation-transcription coupling caused by CREB (cyclic adenosine monophosphate-responsive element-binding protein) shut-off and nuclear accumulation of class IIa histone deacetylases. Interdependency within the triad fuels an accelerating disease progression that culminates in failure of mitochondrial energy production and cell loss...
February 16, 2017: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/28208711/antidepressant-effects-of-aripiprazole-augmentation-for-cilostazol-treated-mice-exposed-to-chronic-mild-stress-after-ischemic-stroke
#4
Yu Ri Kim, Ha Neui Kim, Ki Whan Hong, Hwa Kyoung Shin, Byung Tae Choi
The aim of this study was to determine the effects and underlying mechanism of aripiprazole (APZ) augmentation for cilostazol (CLS)-treated post-ischemic stroke mice that were exposed to chronic mild stress (CMS). Compared to treatment with either APZ or CLS alone, the combined treatment resulted in a greater reduction in depressive behaviors, including anhedonia, despair-like behaviors, and memory impairments. This treatment also significantly reduced atrophic changes in the striatum, cortex, and midbrain of CMS-treated ischemic mice, and inhibited neuronal cell apoptosis, particularly in the striatum and the dentate gyrus of the hippocampus...
February 8, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28202681/components-of-the-mitochondrial-camp-signalosome
#5
REVIEW
Stefania Monterisi, Manuela Zaccolo
3'-5'-Cyclic adenosine monophosphate/protein kinase A (cAMP/PKA) signalling is activated by different extracellular stimuli and mediates many diverse processes within the same cell. It is now well established that in order to translate into the appropriate cellular function multiple extracellular inputs, which may act simultaneously on the same cell, the cAMP/PKA signalling pathway is compartmentalised. Multimolecular complexes are organised at specific subcellular sites to generate spatially confined signalosomes, which include effectors, modulators and targets of the pathway...
February 8, 2017: Biochemical Society Transactions
https://www.readbyqxmd.com/read/28197194/cortical-regulation-of-striatal-projection-neurons-and-interneurons-in-a-parkinson-s-disease-rat-model
#6
Jia-Jia Wu, Si Chen, Li-Si Ouyang, Yu Jia, Bing-Bing Liu, Shu-Hua Mu, Yu-Xin Ma, Wei-Ping Wang, Jia-You Wei, You-Lan Li, Zhi Chen, Wan-Long Lei
Striatal neurons can be either projection neurons or interneurons, with each type exhibiting distinct susceptibility to various types of brain damage. In this study, 6-hydroxydopamine was injected into the right medial forebrain bundle to induce dopamine depletion, and/or ibotenic acid was injected into the M1 cortex to induce motor cortex lesions. Immunohistochemistry and western blot assay showed that dopaminergic depletion results in significant loss of striatal projection neurons marked by dopamine- and cyclic adenosine monophosphate-regulated phosphoprotein, molecular weight 32 kDa, calbindin, and μ-opioid receptor, while cortical lesions reversed these pathological changes...
December 2016: Neural Regeneration Research
https://www.readbyqxmd.com/read/28194663/cilostazol-use-is-associated-with-reduced-risk-of-dementia-a-nationwide-cohort-study
#7
Shu-Yu Tai, Chen-Yu Chien, Yu-Han Chang, Yuan-Han Yang
Whether antiplatelet agents have a preventive effect on cognitive function remains unknown. We examined the potential association between the use of cilostazol, an antiplatelet agent and cyclic adenosine monophosphate phosphodiesterase 3 inhibitor, and the risk of dementia in an Asian population. Patients initiating cilostazol therapy between 1 January 2004 and 31 December 2009 without a prior history of dementia were identified from Taiwan's National Health Insurance database. Participants were stratified by age, sex, comorbidities, and comedication...
February 13, 2017: Neurotherapeutics: the Journal of the American Society for Experimental NeuroTherapeutics
https://www.readbyqxmd.com/read/28182666/direct-protein-introduction-into-plant-cells-using-a-multi-gas-plasma-jet
#8
Yuki Yanagawa, Hiroaki Kawano, Tomohiro Kobayashi, Hidekazu Miyahara, Akitoshi Okino, Ichiro Mitsuhara
Protein introduction into cells is more difficult in plants than in mammalian cells, although it was reported that protein introduction was successful in shoot apical meristem and leaves only together with a cell-penetrating peptide. In this study, we tried to introduce superfolder green fluorescent protein (sGFP)-fused to adenylate cyclase as a reporter protein without a cell-penetrating peptide into the cells of tobacco leaves by treatment with atmospheric non-thermal plasmas. For this purpose, CO2 or N2 plasma was generated using a multi-gas plasma jet...
2017: PloS One
https://www.readbyqxmd.com/read/28181555/determination-of-biological-activity-of-gonadotropins-hcg-and-fsh-by-f%C3%A3-rster-resonance-energy-transfer-based-biosensors
#9
Olga Mazina, Anni Allikalt, Juha S Tapanainen, Andres Salumets, Ago Rinken
Determination of biological activity of gonadotropin hormones is essential in reproductive medicine and pharmaceutical manufacturing of the hormonal preparations. The aim of the study was to adopt a G-protein coupled receptor (GPCR)-mediated signal transduction pathway based assay for quantification of biological activity of gonadotropins. We focussed on studying human chorionic gonadotropin (hCG) and follicle-stimulating hormone (FSH), as these hormones are widely used in clinical practice. Receptor-specific changes in cellular cyclic adenosine monophosphate (cAMP, second messenger in GPCR signalling) were monitored by a Förster resonance energy transfer (FRET) biosensor protein (T)Epac(VV) in living cells upon activation of the relevant gonadotropin receptor...
February 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28179252/aquaporin-2-membrane-targeting-still-a-conundrum
#10
Emma Tina Bisgaard Olesen, Robert A Fenton
The targeting of the water channel aquaporin-2 (AQP2) to the apical plasma membrane of kidney collecting duct principal cells is regulated mainly by the antidiuretic peptide hormone arginine vasopressin (AVP). This process is of crucial importance for the maintenance of body water homeostasis. In this brief review we assess the role of cyclic adenosine monophosphate (cAMP) and discuss the emerging concept that V2R-mediated AQP2 trafficking is cAMP-independent.
February 8, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28174522/in-vivo-imaging-of-mitochondrial-transport-in-single-axon-regeneration-of-zebrafish-mauthner-cells
#11
Yang Xu, Min Chen, Bingbing Hu, Rongchen Huang, Bing Hu
Mitochondrial transport is essential for neuronal function, but the evidence of connections between mitochondrial transport and axon regeneration in the central nervous system (CNS) of living vertebrates remains limited. Here, we developed a novel model to explore mitochondrial transport in a single Mauthner axon (M axon) of zebrafish with non-invasive in vivo imaging. To confirm the feasibility of using this model, we treated labeled zebrafish with nocodazole and demonstrated that it could disrupt mitochondrial transport...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28161696/l-carnitine-ameliorates-the-decrease-of-aquaporin-2-levels-in-rats-with-cisplatin-induced-kidney-injury
#12
Jianjun Gao, Zhaoyan Gu, Min Li, Yongxing Xu, Yuehua Gao, Jiamei Wei, Boran Liang, Yu Na
BACKGROUND: It has been found that L-carnitine ameliorated cisplatin-induced acute kidney injury (AKI) in rats. However, the detailed role of L-carnitine in improving the renal urinary concentration function in cisplatin-induced AKI is not fully understood. METHODS: In this study, 30 Sprague-Dawley rats were divided randomly into 5 groups: control, cisplatin (CIS), L-carnitine (CAR), L-carnitine plus cisplatin (CAR + CIS), and cisplatin plus L-carnitine (CIS + CAR) groups...
February 4, 2017: Nephron
https://www.readbyqxmd.com/read/28154525/deletion-of-type-3-adenylyl-cyclase-perturbs-the-postnatal-maturation-of-olfactory-sensory-neurons-and-olfactory-cilium-ultrastructure-in-mice
#13
Zhe Zhang, Dong Yang, Mengdi Zhang, Ning Zhu, Yanfen Zhou, Daniel R Storm, Zhenshan Wang
Type 3 adenylyl cyclase (Adcy3) is localized to the cilia of olfactory sensory neurons (OSNs) and is an essential component of the olfactory cyclic adenosine monophosphate (cAMP) signaling pathway. Although the role of this enzyme in odor detection and axonal projection in OSNs was previously characterized, researchers will still have to determine its function in the maturation of postnatal OSNs and olfactory cilium ultrastructure. Previous studies on newborns showed that the anatomic structure of the main olfactory epithelium (MOE) of Adcy3 knockout mice (Adcy3(-/-)) is indistinguishable from that of their wild-type littermates (Adcy3(+/+)), whereas the architecture and associated composition of MOE are relatively underdeveloped at this early age...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28152402/molecular-cloning-tissue-distribution-and-pharmacological-characterization-of-melanocortin-4-receptor-in-grass-carp-ctenopharyngodon-idella
#14
L Li, Z Yang, Y-P Zhang, S He, X-F Liang, Y-X Tao
Melanocortin-4 receptor (MC4R) plays a pivotal role in the mediation of leptin action on food intake and energy expenditure in mammals. The MC4R has also been identified in several teleosts, and its importance in the regulation of fish energy homeostasis is emerging. We herein reported on the molecular cloning, tissue distribution, and pharmacological characterization of MC4R in grass carp (Ctenopharyngodon idella), an economically and ecologically important fish. We showed that grass carp MC4R (ciMC4R) consisted of a 981 bp open reading frame encoding a protein of 326 amino acids, highly homologous (>95%) to several teleost MC4Rs...
November 21, 2016: Domestic Animal Endocrinology
https://www.readbyqxmd.com/read/28150511/investigation-of-pde5-pde6-and-pde5-pde11-selective-potent-tadalafil-like-pde5-inhibitors-using-combination-of-molecular-modeling-approaches-molecular-fingerprint-based-virtual-screening-protocols-and-structure-based-pharmacophore-development
#15
Gülru Kayık, Nurcan Ş Tüzün, Serdar Durdagi
The essential biological function of phosphodiesterase (PDE) type enzymes is to regulate the cytoplasmic levels of intracellular second messengers, 3',5'-cyclic guanosine monophosphate (cGMP) and/or 3',5'-cyclic adenosine monophosphate (cAMP). PDE targets have 11 isoenzymes. Of these enzymes, PDE5 has attracted a special attention over the years after its recognition as being the target enzyme in treating erectile dysfunction. Due to the amino acid sequence and the secondary structural similarity of PDE6 and PDE11 with the catalytic domain of PDE5, first-generation PDE5 inhibitors (i...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28130732/zebrafish-phosvitin-derived-peptide-pt5-inhibits-melanogenesis-via-camp-pathway
#16
Yuan-Yuan Liu, Xiu-Rong Su, Shou-Sheng Liu, Shuang-Shuang Yang, Cheng-Yan Jiang, Yu Zhang, Shicui Zhang
Zebrafish phosvitin-derived peptide Pt5, consisting of the C-terminal 55 residues of phosvitin, has been shown to have an antimicrobial-immunomodulatory activity comparable to phosvitin. Here, we showed clearly that Pt5 had the capacity to inhibit tyrosinase (TYR) activity and melanin biosynthesis, and this inhibition was independent of cell proliferation and cytotoxic effects. Incubation of fluorescein isothiocyanate (FITC)-labeled Pt5 with B16F10 melanoma cells revealed that Pt5 was localized in the cytoplasm of the cells...
January 27, 2017: Fish Physiology and Biochemistry
https://www.readbyqxmd.com/read/28126553/korean-red-ginseng-improves-testicular-ineffectiveness-in-aging-rats-by-modulating-spermatogenesis-related-molecules
#17
Spandana Rajendra Kopalli, Kyu-Min Cha, Ji-Hoon Ryu, Sang-Ho Lee, Min-Sik Jeong, Seock-Yeon Hwang, Young-Joo Lee, Hee-Won Song, Su-Nam Kim, Jin-Chul Kim, Si-Kwan Kim
Korean red ginseng (Panax ginseng Meyer) is known to rejuvenate testicular effectiveness and the sperm maturation process by regulating redox proteins in aged rats. This study was performed to investigate the effect of Korean red ginseng water extract (KRG-WE) on the expression level of spermatogenesis-related key biomolecules and sex hormone receptors as well as enzymes regulating oxidation, histone deacetylation, and growth-related activities in aged rat testis. KRG-WE (200mg/kg) mixed with a regular pellet diet was administered to 12-month-old rats for 6months (KRG-AC), whereas the young (YC, 2months) and aged (AC, 12months) controls received the vehicle only...
January 23, 2017: Experimental Gerontology
https://www.readbyqxmd.com/read/28124089/evening-primrose-oil-or-forskolin-ameliorates-celecoxib-enhanced-upregulation-of-tissue-factor-expression-in-mice-subjected-to-lipopolysaccharide-induced-endotoxemia
#18
Sarah M Mosaad, Sawsan A Zaitone, Amal A M Ahmed, Dina M Abo-Elmatty, Amani A El-Baz, Yasser M Moustafa
Celecoxib, a selective cyclooxygenase-2 inhibitor, produces thrombotic events in patients predisposed to cardiovascular risk factors. One theory reported an increase in endothelial expression of tissue factor (TF) as a predisposing factor. This work explored the effect of evening primrose oil (EPO), a source of prostaglandin E1, and forskolin (a cyclic adenosine monophosphate stimulator) against the prothrombotic effect of celecoxib in mice. Lipopolysaccharide mouse model of endotoxemia was used to induce an upregulation of TF activity...
January 26, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28123632/effects-of-averrhoa-carambola-l-oxalidaceae-juice-mediated-on-hyperglycemia-hyperlipidemia-and-its-influence-on-regulatory-protein-expression-in-the-injured-kidneys-of-streptozotocin-induced-diabetic-mice
#19
Hoa Thi Thai Pham, Wansu Huang, Chuangye Han, Juman Li, Qiuqiao Xie, Jinbin Wei, Xiaohui Xu, Zefeng Lai, Xiang Huang, Renbin Huang, Qingwei Wen
Recently, many reports have shown that Averrhoa carambola L. (Oxalidaceae) juice (EACJ) could reduce blood glucose in humans. However, its mechanisms have not been well explored; therefore, our study aimed to investigate the beneficial effects of EACJ on hyperglycemia, hyperlipidemia and renal injury in streptozotocin (STZ)-induced diabetic mice. Those mice were injected with STZ via the tail vein (120 mg/kg body weight) and were identified as diabetic mice when the level of blood glucose was ≥ 11.1 mmol/L...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28119465/phosphorylation-of-ser1928-mediates-the-enhanced-activity-of-the-l-type-ca2-channel-cav1-2-by-the-%C3%AE-2-adrenergic-receptor-in-neurons
#20
Hai Qian, Tommaso Patriarchi, Jennifer L Price, Lucas Matt, Boram Lee, Madeline Nieves-Cintrón, Olivia R Buonarati, Dhrubajyoti Chowdhury, Evanthia Nanou, Matthew A Nystoriak, William A Catterall, Montatip Poomvanicha, Franz Hofmann, Manuel F Navedo, Johannes W Hell
The L-type Ca(2+) channel Cav1.2 controls multiple functions throughout the body including heart rate and neuronal excitability. It is a key mediator of fight-or-flight stress responses triggered by a signaling pathway involving β-adrenergic receptors (βARs), cyclic adenosine monophosphate (cAMP), and protein kinase A (PKA). PKA readily phosphorylates Ser(1928) in Cav1.2 in vitro and in vivo, including in rodents and humans. However, S1928A knock-in (KI) mice have normal PKA-mediated L-type channel regulation in the heart, indicating that Ser(1928) is not required for regulation of cardiac Cav1...
January 24, 2017: Science Signaling
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