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https://www.readbyqxmd.com/read/28107736/crystal-structures-binding-interactions-and-adme-evaluation-of-brain-penetrant-n-substituted-indazole-5-carboxamides-as-subnanomolar-selective-monoamine-oxidase-b-and-dual-mao-a-b-inhibitors
#1
Nikolay T Tzvetkov, Hans-Georg Stammler, Beate Neumann, Silvia Hristova, Liudmil Antonov, Marcus Gastreich
The pharmacological and physicochemical analysis of structurally optimized N-alkyl-substituted indazole-5-carboxamides, developed as potential drug and radioligand candidates for the treatment and diagnosis of Parkinson's disease (PD) and other neurological disorders, is reported. Recent efforts have been focused on the development of subnanomolar potent, selective MAO-B (N1-alkyl-substituted compounds 12a-14a and 15) and dual active MAO-A/B (N2-methylated compounds 12b-14b) inhibitors with nanomolar potency towards MAO-B and moderately active against MAO-A enzyme, respectively...
January 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28105278/hydrazone-linker-as-a-useful-tool-for-preparing-chimeric-peptide-nonpeptide-bifunctional-compounds
#2
Jolanta Dyniewicz, Piotr F J Lipiński, Piotr Kosson, Anna Leśniak, Marta Bochyńska-Czyż, Adriana Muchowska, Dirk Tourwé, Steven Ballet, Aleksandra Misicka, Andrzej W Lipkowski
The area of multitarget compounds, joining two pharmacophores within one molecule, is a vivid field of research in medicinal chemistry. Not only pharmacophoric elements are essential for the design and activity of such compounds, but the type and length of linkers used to connect them are also crucial. In the present contribution, we describe compound 1 in which a typical opioid peptide sequence is combined with a fragment characteristic for neurokinin-1 receptor (NK1R) antagonists through a hydrazone bridge...
January 12, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28105094/protective-effect-of-geraniol-inhibits-inflammatory-response-oxidative-stress-and-apoptosis-in-traumatic-injury-of-the-spinal-cord-through-modulation-of-nf-%C3%AE%C2%BAb-and-p38-mapk
#3
Jiansheng Wang, Baishan Su, Hongbin Zhu, Chao Chen, Gang Zhao
Geraniol is a type of monoterpenoid with a rose scent and a slightly sweet flavor. It is found in the volatile oil of various plants, and has anti-inflammatory and anti-oxidant effects. The present study aimed to investigate the protective effect of geraniol in inhibiting the inflammatory response, oxidative stress and apoptosis in traumatic spinal cord injury (SCI), as well as to analyze the mechanism underlying its effect. Adult male Sprague-Dawley rats were induced to traumatic SCI through a surgical procedure and were defined as the SCI model group...
December 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28101766/crossing-the-blood-brain-barrier-recent-advances-in-drug-delivery-to-the-brain
#4
Mayur M Patel, Bhoomika M Patel
CNS disorders are on the rise despite advancements in our understanding of their pathophysiological mechanisms. A major hurdle to the treatment of these disorders is the blood-brain barrier (BBB), which serves as an arduous janitor to protect the brain. Many drugs are being discovered for CNS disorders, which, however fail to enter the market because of their inability to cross the BBB. This is a pronounced challenge for the pharmaceutical fraternity. Hence, in addition to the discovery of novel entities and drug candidates, scientists are also developing new formulations of existing drugs for brain targeting...
January 18, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28098771/breast-cancer-brain-metastases-clonal-evolution-in-clinical-context
#5
REVIEW
Jodi M Saunus, Amy E McCart Reed, Zhun Leong Lim, Sunil R Lakhani
Brain metastases are highly-evolved manifestations of breast cancer arising in a unique microenvironment, giving them exceptional adaptability in the face of new extrinsic pressures. The incidence is rising in line with population ageing, and use of newer therapies that stabilise metastatic disease burden with variable efficacy throughout the body. Historically, there has been a widely-held view that brain metastases do not respond to circulating therapeutics because the blood-brain-barrier (BBB) restricts their uptake...
January 13, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28098158/pericytes-from-mesenchymal-stem-cells-as-a-model-for-the-blood-brain-barrier
#6
Xiaohe Tian, Oliver Brookes, Giuseppe Battaglia
Blood brain-barrier (BBB) in vitro models have been widely reported in studies of the BBB phenotype. However, established co-culture systems involve brain endothelial cells, astrocytes, neurons and pericytes, and therefore are often consuming and technically challenging. Here we use mesenchymal system cells (MSC) as a potential substitute for pericytes in a BBB model. Both MSC and pericyte markers in 2D culture environment were evaluated on different extracellular matrix compositions. Further experiments indicated that MSC contributed in a similar manner to pericytes in a co-cultured 3D model on increasing trans-endothelial electric resistance (TEER) and decreasing permeability against macromolecules...
January 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28097491/small-interfering-rna-targeting-dickkopf-1-contributes-to-neuroprotection-after-intracerebral-hemorrhage-in-rats
#7
Zhihua Li, Xi Chen, Xiaoyang Zhang, Xiuhua Ren, Xuemei Chen, Jing Cao, Weidong Zang, Xianzhi Liu, Fuyou Guo
Excessive Dickkopf-1 (Dkk-1) plays a vital role in secondary brain injury following ischemic stroke and psychotic disease. However, it is unclear whether an increased expression of Dkk-1 occurred after intracerebral hemorrhage (ICH). The present study examined the potential role of Dkk-1 after ICH. ICH was induced by a single injection of autologous blood into the basal ganglia of rats. Dkk-1 protein levels in brain tissue and serum were detected by enzyme-linked immunosorbent assay after ICH. Rats were treated with small interfering RNA targeting Dkk-1 (siDkk-1) or vehicle following ICH...
January 17, 2017: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/28097067/anatomical-mechanism-of-spontaneous-recovery-in-regions-caudal-to-thoracic-spinal-cord-injury-lesions-in-rats
#8
Lu-Sheng Li, Hao Yu, Raynald Raynald, Xiao-Dong Wang, Guang-Hui Dai, Hong-Bin Cheng, Xue-Bin Liu, Yi-Hua An
BACKGROUND: The nerve fibre circuits around a lesion play a major role in the spontaneous recovery process after spinal cord hemisection in rats. The aim of the present study was to answer the following question: in the re-control process, do all spinal cord nerves below the lesion site participate, or do the spinal cord nerves of only one vertebral segment have a role in repair? METHODS: First we made a T7 spinal cord hemisection in 50 rats. Eight weeks later, they were divided into three groups based on distinct second operations at T7: ipsilateral hemisection operation, contralateral hemisection, or transection...
2017: PeerJ
https://www.readbyqxmd.com/read/28094184/in-vivo-evaluation-of-igf1r-ir-pet-ligand-18-f-bms-754807-in-rodents
#9
Jaya Prabhakaran, Stephen L Dewey, Richard McClure, Norman R Simpson, Mohammed N Tantawy, J John Mann, Wellington Pham, J S Dileep Kumar
In vivo evaluation of [(18)F]BMS-754807 binding in mice and rats using microPET and biodistribution methods is described herein. The radioligand shows consistent binding characteristics, in vivo, in both species. Early time frames of the microPET images and time activity curves of brain indicate poor penetration of the tracer across the blood brain barrier (BBB) in both species. However, microPET experiments in mice and rats show high binding of the radioligand outside the brain to heart, pancreas and muscle, the organs known for higher expression of IGF1R/1R...
January 7, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28093570/vitamin-d-administration-cognitive-function-bbb-permeability-and-neuro-inflammatory-factors-in-high-fat-diet-induced-obese-rats
#10
G Hajiluian, G Nameni, P Shahabi, M Mesgari-Abbasi, S Sadigh-Eteghad, M A Farhangi
OBJECTIVES: The purpose of this research is to investigate the effects of vitamin D administration on cognitive function, nuclear factor Kappa-B (NF-kB), brain derived neurotrophic factor (BDNF) concentration in the hippocampus and blood-brain barrier (BBB) permeability in high-fat diet (HFD) induced obese rats. METHODS: Male Wistar rats were fed either a control diet or HFD for 16 weeks (n=20); then each group was randomized into two subgroups supplemented orally with 500 IU/kg vitamin D for 5 weeks...
January 17, 2017: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/28093288/assessing-the-impact-of-lithium-chloride-on-the-expression-of-p-glycoprotein-at-the-blood-brain-barrier
#11
Stephanie A Newman, Yijun Pan, Jennifer L Short, Joseph A Nicolazzo
In addition to extruding drugs from the brain, P-glycoprotein (P-gp) at the blood-brain barrier (BBB) facilitates the brain-to-blood clearance of β-amyloid (Aβ) and is down-regulated in Alzheimer's disease (AD). Studies suggest that the mood-stabilising drug lithium exerts a protective effect against AD. While the mechanisms underlying this effect are not fully understood, evidence suggests that lithium chloride (LiCl) increases P-gp expression in vitro, albeit at concentrations substantially outside the therapeutic window...
January 13, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28092082/brain-barrier-breakdown-as-a-cause-and-consequence-of-neuroinflammation-in-sepsis
#12
REVIEW
Lucineia Gainski Danielski, Amanda Della Giustina, Marwa Badawy, Tatiana Barichello, João Quevedo, Felipe Dal-Pizzol, Fabrícia Petronilho
The blood-brain barrier (BBB) and the blood-cerebrospinal fluid barrier (BCSFB) are important for the maintenance of brain homeostasis. During sepsis, peripheral production of proinflammatory cytokines and reactive oxygen species are responsible for structural alterations in those brain barriers. Thus, an increasing permeability of these barriers can lead to the activation of glial cells such as microglia and the production of cytotoxic mediators which in turn act on the brain barriers, damaging them further...
January 14, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28091711/anticholinergic-prescription-are-healthcare-professionals-the-real-burden
#13
George Araklitis, Ganesh Thiagamoorthy, Jo Hunter, Angie Rantell, Dudley Robinson, Linda Cardozo
INTRODUCTION AND HYPOTHESIS: Anticholinergic medication is the medical treatment for overactive bladder (OAB). These drugs can act on the central nervous system and can lead to cognitive decline, dementia, and potentially death. Patients taking drugs with anticholinergic effects increase their anticholinergic burden-defined as the cumulative effect of taking one or more drugs that can have adverse effects. When prescribing anticholinergic medication for the elderly, we must choose the right drug...
January 13, 2017: International Urogynecology Journal
https://www.readbyqxmd.com/read/28091411/protective-effects-of-calpain-inhibition-on-neurovascular-unit-injury-through-downregulating-nuclear-factor-%C3%AE%C2%BAb-related-inflammation-during-traumatic-brain-injury-in-mice
#14
Xiao-Gang Tao, Jing-Hua Shi, Shu-Yu Hao, Xue-Tao Chen, Bai-Yun Liu
BACKGROUND: In addition to neurons, all components of the neurovascular unit (NVU), such as glial, endothelial, and basal membranes, are destroyed during traumatic brain injury (TBI). Previous studies have shown that excessive stimulation of calpain is crucial for cerebral injury after traumatic insult. The objective of this study was to investigate whether calpain activation participated in NVU disruption and edema formation in a mouse model of controlled cortical impact (CCI). METHODS: One hundred and eight mice were divided into three groups: the sham group, the control group, and the MDL28170 group...
2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/28089819/lentivirus-mediated-silencing-of-the-ctgf-gene-suppresses-the-formation-of-glial-scar-tissue-in-a-rat-model-of-spinal-cord-injury
#15
Yuan Wang, Qin-Jie Kong, Jing-Chuan Sun, Yong Yang, Hai-Bo Wang, Qiang Zhang, Jian-Gang Shi
BACKGROUND CONTEXT: - One of the many reactive changes following an Spinal cord injury (SCI) is the formation of a glial scar, a reactive cellular process whereby glial cells accumulate and surround central nervous system (CNS) injury sites to seal in the wound. Thus the inhibition of glial scar is of great importance for SCI recovery. PURPOSE: - This study aimed to explore the effect of lentivirus-mediated silencing of the CTGF gene on the formation of glial scar tissue in a rat model of spinal cord injury (SCI)...
January 9, 2017: Spine Journal: Official Journal of the North American Spine Society
https://www.readbyqxmd.com/read/28089577/neutralizing-anti-interleukin-1%C3%AE-antibodies-reduce-ischemia-related-interleukin-1%C3%AE-transport-across-the-blood-brain-barrier-in-fetal-sheep
#16
Aparna Patra, Xiaodi Chen, Grazyna B Sadowska, Jiyong Zhang, Yow-Pin Lim, James F Padbury, William A Banks, Barbara S Stonestreet
Hypoxic ischemic insults predispose to perinatal brain injury. Pro-inflammatory cytokines are important in the evolution of this injury. Interleukin-1β (IL-1β) is a key mediator of inflammatory responses and elevated IL-1β levels in brain correlate with adverse neurodevelopmental outcomes after brain injury. Impaired blood-brain barrier (BBB) function represents an important component of hypoxic-ischemic brain injury in the fetus. In addition, ischemia-reperfusion increases cytokine transport across the BBB of the ovine fetus...
January 9, 2017: Neuroscience
https://www.readbyqxmd.com/read/28089093/minimally-invasive-surgery-for-evacuating-the-intracerebral-hematoma-in-early-stages-decreased-secondary-damages-to-the-internal-capsule-in-dog-model-of-ich-observed-by-diffusion-tensor-imaging
#17
Guofeng Wu, Fan Wang, Likun Wang, Jing Shi, Hui Yu, Yingjun Zhang
BACKGROUND: Diffusion tensor imaging was used to observe the effects of performing early minimally invasive surgery (MIS) on internal capsule in dog model of intracerebral hemorrhage (ICH). METHODS: Twenty-five male dogs were selected to prepare an ICH model, and then they were randomly distributed into a model control (MC) group (5 dogs) or an MIS group (20 dogs). In the MIS group, the intracerebral hematoma was evacuated by stereotactic minimally invasive procedures over 6 hours (5 dogs), 12 hours (5 dogs), 18 hours (5 dogs), or 24 hours (5 dogs) after successful induction of ICH...
January 6, 2017: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/28088972/-critical-roles-of-matrix-metalloproteinases-secreted-by-leukemic-cells-in-the-pathogenesis-of-central-nervous-system-leukemia
#18
S R Feng, Z X Chen, J N Cen, H J Shen, Y Y Wang, L Yao
Objective: To observe the effects of matrix metalloproteinases (MMP)-2 and MMP-9 secreted by leukemic cells on tight junction proteins ZO-1, claudin-5 and occluding and the permeability of the blood-brain barrier (BBB) and explore the mechanisms of MMP-2 and MMP-9 in leukemic cell infiltration of the central nervous system (CNS). Methods: The mRNA expressions of MMP-2 and MMP-9 in leukemic cell lines SHI-1, HL-60 and U937 were detected by quantitative RT-PCR. The MMP inhibitor GM6001 was used to inhibit the secretion of MMP-2 and MMP-9...
December 14, 2016: Zhonghua Xue Ye Xue za Zhi, Zhonghua Xueyexue Zazhi
https://www.readbyqxmd.com/read/28088914/diverse-functions-and-mechanisms-of-pericytes-in-ischemic-stroke
#19
Shuai Yang, Huijuan Jin, Yiyi Zhu, Yan Wan, Lingqiang Zhu, Bo Hu
Pericytes are mural cells embedded in the basement membrane of microvessels. Because of such a unique position in the blood-brain barrier (BBB) and neurovascular unit (NVU), they receive, orchestrate and process signals from their neighboring cells to generate diverse neurovascular functions, including regulation of capillary hemodynamics, BBB permeability, clearance of toxic metabolites, angiogenesis, neuroinflammation and stem cell activity. During the different stages of ischemic stroke, pericytes play different roles: 1) On the hyperacute phase of stroke, pericytes constriction and death may be a cause of the no-reflow phenomenon in brain capillaries; 2) During the acute phase, pericytes detach from microvessels and participate in inflammatory-immunological response, resulting in the BBB damage and brain edema...
January 12, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28088890/nanoparticles-as-a-carrier-system-for-drug-delivery-across-blood-brain-barrier
#20
Alika Sarkar, Ismat Fatima, Qazi Mohammad Sajid Jamal, Usman Sayeed, M Kalim A Khan, Salman Akhtar, Mohammad Amjad Kamal, Alvina Farooqui, Mohammad Haris Siddiqui
Brain, the center of the nervous system and an integral part the body, is protected by two anatomical and biochemical dynamic barriers- Blood-Brain Barrier (BBB) and Blood-Cerebrospinal Fluid Barrier (BCSFB). Blood-Brain Barrier is a highly complex multi-cellular organized structure that protects the brain from harmful substances and invading organisms from the bloodstream and thus protecting it from diseases and injuries. However, it also significantly precludes the delivery of drug to the brain, thus, preventing treatment of a number of neurological disorders...
January 13, 2017: Current Drug Metabolism
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