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Skeletal muscle relaxant

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https://www.readbyqxmd.com/read/27904817/transitional-vertebra-and-spina-bifida-occulta-related-with-chronic-low-back-pain-in-a-young-patient
#1
Maryam Kundi, Maham Habib, Sumbal Babar, Asif K Kundi, Salman Assad, Amjad Sheikh
Bertolotti's syndrome (BS) must be considered as a differential diagnosis in a young patient presenting with low back pain (LBP). We present a case of a 26-year-old male complaining of mild chronic LBP for six years, radiating to his left thigh for the past six months. He has been taking non-steroidal anti-inflammatory drugs (NSAIDs) with skeletal muscle relaxants for pain relief. The X-ray and computed tomography (CT) imagings showed congenital enlargement of the left transverse process of the fifth lumbar (L5) vertebra forming pseudo-articulation with the sacrum and unilateral pars interarticularis defect at the L4 level on the left side, respectively...
October 19, 2016: Curēus
https://www.readbyqxmd.com/read/27879676/calcium-dyshomeostasis-in-tubular-aggregate-myopathy
#2
REVIEW
Jong-Mok Lee, Satoru Noguchi
Calcium is a crucial mediator of cell signaling in skeletal muscles for basic cellular functions and specific functions, including contraction, fiber-type differentiation and energy production. The sarcoplasmic reticulum (SR) is an organelle that provides a large supply of intracellular Ca(2+) in myofibers. Upon excitation, it releases Ca(2+) into the cytosol, inducing contraction of myofibrils. During relaxation, it takes up cytosolic Ca(2+) to terminate the contraction. During exercise, Ca(2+) is cycled between the cytosol and the SR through a system by which the Ca(2+) pool in the SR is restored by uptake of extracellular Ca(2+) via a specific channel on the plasma membrane...
November 22, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27879195/the-pharmacokinetic-comparison-and-bioequivalence-evaluation-of-two-10-mg-baclofen-formulations-in-healthy-male-subjects%C3%A2
#3
Sumin Yoon, SeungHwan Lee, Kyung-Sang Yu, Sung-Vin Yim, Bo-Hyung Kim
BACKGROUNDS: Baclofen is used as a skeletal muscle relaxant for multiple sclerosis patients. It depresses the transmission of monosynaptic and polysynaptic reflex by stimulating GABAβ (gamma-aminobutyric acid) receptors. OBJECTIVES: The aim of this study was to compare the pharmacokinetic characteristics of two 10-mg baclofen formulations and to assess bioequivalence. METHODS: A randomized, single-dose, two-period, two-sequence crossover study was conducted in healthy male subjects...
November 23, 2016: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27869319/the-ca-2-sensitizer-ck-2066260-increases-myofibrillar-ca-2-sensitivity-and-submaximal-force-selectively-in-fast-skeletal-muscle
#4
Darren T Hwee, Arthur J Cheng, James J Hartman, Aaron C Hinken, Ken Lee, Nickie Durham, Alan J Russell, Fady I Malik, Håkan Westerblad, Jeffrey R Jasper
Skeletal muscle dysfunction occurs in many diseases and can lead to muscle weakness and premature muscle fatigue. Here we show that the fast skeletal troponin activator, CK-2066260, counteracts muscle weakness by increasing troponin Ca(2+) affinity, thereby increasing myofibrillar Ca(2+) sensitivity. Exposure to CK-2066260 resulted in a concentration-dependent increase in the Ca(2+) sensitivity of ATPase activity in isolated myofibrils and reconstituted hybrid sarcomeres containing fast skeletal muscle troponin C...
November 21, 2016: Journal of Physiology
https://www.readbyqxmd.com/read/27862560/noninvasive-assessment-of-age-gender-and-exercise-effects-on-skeletal-muscle-initial-experience-with-t1-%C3%AF-mri-of-calf-muscle
#5
Xin-Gui Peng, Yuancheng Wang, Shijun Zhang, Yingying Bai, Hui Mao, Gao-Jun Teng, Shenghong Ju
PURPOSE: To prospectively investigate age- and gender-related changes in the fast-twitch (tibialis anterior, TA) and slow-twitch (soleus, SOL) skeletal muscle of healthy rats and volunteers and to compare the exercise-related difference in health volunteers with T1 ρ magnetic resonance imaging (MRI). MATERIALS AND METHODS: In all, 18 rats and 70 humans were involved in this study. For the animal study, T1 ρ relaxation times were measured in the TA and SOL rat muscle with a 3...
November 9, 2016: Journal of Magnetic Resonance Imaging: JMRI
https://www.readbyqxmd.com/read/27861245/selective-impairment-of-blood-pressure-reduction-by-endothelial-nitric-oxide-synthase-dimer-destabilization-in-mice
#6
Tatsiana Suvorava, Stephanie Pick, Georg Kojda
OBJECTIVES: Endothelial dysfunction and oxidative stress are associated with hypertension but whether endothelial superoxide may play a role in the early development of essential hypertension remains uncertain. We investigated whether endothelial nitric oxide synthase (eNOS)-derived endothelial oxidative stress is involved in the regulation of SBP. METHODS: Wild-type eNOS [mice with endothelium-specific overexpression of bovine endothelial NO-synthase (eNOS-Tg)] or a novel dimer-destabilized eNOS-mutant harboring a partially disrupted zinc-finger [mice with endothelium-specific overexpression of destabilized bovine eNOS destabilized by replacement of Cys 101 to Ala (C101A-eNOS-Tg)] was introduced in C57BL/6 in an endothelial-specific manner...
January 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/27857962/functional-analysis-of-ryr1-variants-linked-to-malignant-hyperthermia
#7
Jeremy Stephens, Anja H Schiemann, Cornelia Roesl, Dorota Miller, Sean Massey, Neil Pollock, Terasa Bulger, Kathryn Stowell
Malignant hyperthermia manifests as a rapid and sustained rise in temperature in response to pharmacological triggering agents, e.g. inhalational anesthetics and the muscle relaxant suxamethonium. Other clinical signs include an increase in end-tidal CO2, increased O2 consumption, as well as tachycardia, and if untreated a malignant hyperthermia episode can result in death. The metabolic changes are caused by dysregulation of skeletal muscle Ca(2+) homeostasis, resulting from a defective ryanodine receptor Ca(2+) channel, which resides in the sarcoplasmic reticulum and controls the flux of Ca(2+) ions from intracellular stores to the cytoplasm...
April 2016: Temperature: Multidisciplinary Biomedical Journal
https://www.readbyqxmd.com/read/27815532/highly-selective-inhibition-of-myosin-motors-provides-the-basis-of-potential-therapeutic-application
#8
Serena Sirigu, James J Hartman, Vicente José Planelles-Herrero, Virginie Ropars, Sheila Clancy, Xi Wang, Grace Chuang, Xiangping Qian, Pu-Ping Lu, Edward Barrett, Karin Rudolph, Christopher Royer, Bradley P Morgan, Enrico A Stura, Fady I Malik, Anne M Houdusse
Direct inhibition of smooth muscle myosin (SMM) is a potential means to treat hypercontractile smooth muscle diseases. The selective inhibitor CK-2018571 prevents strong binding to actin and promotes muscle relaxation in vitro and in vivo. The crystal structure of the SMM/drug complex reveals that CK-2018571 binds to a novel allosteric pocket that opens up during the "recovery stroke" transition necessary to reprime the motor. Trapped in an intermediate of this fast transition, SMM is inhibited with high selectivity compared with skeletal muscle myosin (IC50 = 9 nM and 11,300 nM, respectively), although all of the binding site residues are identical in these motors...
November 4, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27799519/piperine-s-mitigation-of-obesity-and-diabetes-can-be-explained-by-its-up-regulation-of-the-metabolic-rate-of-resting-muscle
#9
Leonardo Nogara, Nariman Naber, Edward Pate, Marcella Canton, Carlo Reggiani, Roger Cooke
We identify a target for treating obesity and type 2 diabetes, the consumption of calories by an increase in the metabolic rate of resting skeletal muscle. The metabolic rate of skeletal muscle can be increased by shifting myosin heads from the super-relaxed state (SRX), with a low ATPase activity, to a disordered relaxed state (DRX), with a higher ATPase activity. The shift of myosin heads was detected by a change in fluorescent intensity of a probe attached to the myosin regulatory light chain in skinned skeletal fibers, allowing us to perform a high-throughput screen of 2,128 compounds...
November 15, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27793139/a-short-term-statin-treatment-changes-the-contractile-properties-of-fast-twitch-skeletal-muscles
#10
Antoine Boulanger Piette, Sébastien S Dufresne, Jérôme Frenette
BACKGROUND: Cumulative evidence indicates that statins induce myotoxicity. However, the lack of understanding of how statins affect skeletal muscles at the structural, functional, and physiological levels hampers proper healthcare management. The purpose of the present study was to investigate the early after-effects of lovastatin on the slow-twitch soleus (Sol) and fast-twitch extensor digitorum longus (EDL) muscles. METHODS: Adult C57BL/6 mice were orally administrated with placebo or lovastatin [50 mg/kg/d] for 28 days...
October 28, 2016: BMC Musculoskeletal Disorders
https://www.readbyqxmd.com/read/27763660/minimum-number-of-myosin-motors-accounting-for-shortening-velocity-under-zero-load-in-skeletal-muscle
#11
Luca Fusi, Valentina Percario, Elisabetta Brunello, Marco Caremani, Pasquale Bianco, Joseph D Powers, Massimo Reconditi, Vincenzo Lombardi, Gabriella Piazzesi
KEY POINTS: Myosin filament mechanosensing determines the efficiency of the contraction by adapting the number of switched ON motors to the load. Accordingly, the unloaded shortening velocity (V0 ) is already set at the end of the latency relaxation (LR), ∼10 ms after the start of stimulation, when the myosin filament is still in the OFF state. Here the number of actin-attached motors per half-myosin filament (n) during V0 shortening imposed either at the end of LR or at the plateau of the isometric contraction is estimated from the relation between half-sarcomere compliance and force during the force redevelopment after the shortening...
October 20, 2016: Journal of Physiology
https://www.readbyqxmd.com/read/27753838/sy-06-1-obesity-diabetes-and-hypertension-are-adipokines-responsible
#12
Anthony Heagerty
There is now a considerable body of evidence to suggest that the fat cells that surround blood vessels (perivascular adipose tissue, PVAT) can influence profoundly arterial tone by releasing vasodilator adipokines which can act locally in a paracrine fashion. In healthy lean individuals the primary vasodilator released appears to be adiponectin and there is a complex interation between autonomic nerve firing in PVAT and the release of nitric oxide from adipocytes and an increased bioavailability of adiponectin...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27744183/thiadiazolodiazepine-analogues-as-a-new-class-of-neuromuscular-blocking-agents-synthesis-biological-evaluation-and-molecular-modeling-study
#13
Hussein I El-Subbagh, Adel S El-Azab, Ghada S Hassan, Shahenda M El-Messery, Alaa A-M Abdel-Aziz, Kamal E H El-Taher
The synthesis, biological evaluation and molecular modeling study of 6,7-dihydro-[1,3,4] thiadiazolo[3,2-a][1,3]diazepine analogues as new class of neuromuscular blocking agents are described. The new compounds act via competitive mechanism with ACh which could be reversed by the anticholinesterase - Physostigmine. Compounds GS-53 (30) and AAH1 (33) induced dose-dependent neuromuscular blockade with onset time of 3 and 10 min, ED50 0.15 and 0.36 mmol/kg i.p., respectively, in rats. Compound 30 proved to be as twice as potent as 33 with rapid onset and shorter duration (P < 0...
September 30, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27736981/impact-of-tieg1-deletion-on-the-passive-mechanical-properties-of-fast-and-slow-twitch-skeletal-muscles-in-female-mice
#14
Malek Kammoun, Philippe Pouletaut, Francis Canon, Malayannan Subramaniam, John R Hawse, Muriel Vayssade, Sabine F Bensamoun
As transforming growth factor (TGF)-β inducible early gene-1 is highly expressed in skeletal muscle, the effect of TIEG1 gene deletion on the passive mechanical properties of slow and fast twitch muscle fibers was analyzed. Twenty five muscle fibers were harvested from soleus (Sol) and extensor digitorum longus (EDL) muscles from TIEG1-/- (N = 5) and control (N = 5) mice. Mechanical tests were performed on fibers and the dynamic and static stresses were measured. A viscoelastic Hill model of 3rd order was used to fit the experimental relaxation test data...
2016: PloS One
https://www.readbyqxmd.com/read/27725266/complete-primary-structure-of-the-i-band-region-of-connectin-at-which-mechanical-property-is-modulated-in-zebrafish-heart-and-skeletal-muscle
#15
Akira Hanashima, Ken Hashimoto, Yoshihiro Ujihara, Takeshi Honda, Tomoko Yobimoto, Aya Kodama, Satoshi Mohri
Connectin, also called titin, is the largest protein with a critical function as a molecular spring during contraction and relaxation of striated muscle; its mutation leads to severe myopathy and cardiomyopathy. To uncover the cause of this pathogenesis, zebrafish have recently been used as disease models because they are easier to genetically modify than mice. Although the gene structures and putative primary structures of zebrafish connectin have been determined, the actual primary structures of zebrafish connectin in heart and skeletal muscles remain unclear because of its large size and the PCR amplification-associated difficulties...
October 7, 2016: Gene
https://www.readbyqxmd.com/read/27666773/thomsen-disease-with-ptosis-and-abnormal-mr-findings
#16
Yukiko Mori, Satoshi Yamashita, Mai Kato, Teruaki Masuda, Koutaro Takamatsu, Toshihide Kumamoto, Ryogen Sasaki, Yukio Ando
Myotonia congenita is a non-dystrophic skeletal muscle disorder characterized by muscle stiffness and an inability of the muscle to relax after voluntary contraction caused by a mutation in the gene encoding skeletal muscle chloride channel-1 (CLCN1). We encountered a case of Thomsen disease with ptosis. A short tau inversion recovery MR imaging demonstrated high-intensity lesions in the levator palpebrae superioris muscles. Molecular genetic testing revealed a heterozygosity for the c.1439C>A (p.P480H) mutation in the CLCN1 gene...
September 3, 2016: Neuromuscular Disorders: NMD
https://www.readbyqxmd.com/read/27642933/sy-06-1-obesity-diabetes-and-hypertension-are-adipokines-responsible
#17
Anthony Heagerty
There is now a considerable body of evidence to suggest that the fat cells that surround blood vessels (perivascular adipose tissue, PVAT) can influence profoundly arterial tone by releasing vasodilator adipokines which can act locally in a paracrine fashion. In healthy lean individuals the primary vasodilator released appears to be adiponectin and there is a complex interation between autonomic nerve firing in PVAT and the release of nitric oxide from adipocytes and an increased bioavailability of adiponectin...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27640143/tropomyosin-movement-is-described-by-a-quantitative-high-resolution-model-of-x-ray-diffraction-of-contracting-muscle
#18
Natalia A Koubassova, Sergey Y Bershitsky, Michael A Ferenczi, Theyencheri Narayanan, Andrey K Tsaturyan
Contraction of skeletal and cardiac muscle is controlled by Ca(2+) ions via regulatory proteins, troponin (Tn) and tropomyosin (Tpm) associated with the thin actin filaments in sarcomeres. In the absence of Ca(2+), Tn-C binds actin and shifts the Tpm strand to a position where it blocks myosin binding to actin, keeping muscle relaxed. According to the three-state model (McKillop and Geeves Biophys J 65:693-701, 1993), upon Ca(2+) binding to Tn, Tpm rotates about the filament axis to a 'closed state' where some myosin heads can bind actin...
September 17, 2016: European Biophysics Journal: EBJ
https://www.readbyqxmd.com/read/27639708/effect-of-methanol-extract-of-trigonella-foenum-graecum-l-seeds-on-anxiety-sedation-and-motor-coordination
#19
Tahira Assad, Rafeeq Alam Khan
Currently available anxiolytics cause numerous adverse effects and show craving and tolerance during long term treatment. Currently traditional medicines have been re-evaluated widely through work on various plant species. Numerous plants in traditional system show pharmacological activity with unlimited prospective for therapeutic use. Hence we planned to evaluate the effect of methanol extract of T. foenum-graecum L. seeds on anxiety, sedation and motor coordination in mice at different doses following 15 days of oral feeding...
September 17, 2016: Metabolic Brain Disease
https://www.readbyqxmd.com/read/27636876/injuries-in-adults-65-years-of-age-and-older-prescribed-muscle-relaxants
#20
Melissa M Derner, Courtney A Linhart, LeeAnna M Pederson, Sarith M Saju, Alyssa M Heiden, Lisa A Wohlford, Michael T Swanoski, M Nawal Lutfiyya
OBJECTIVE: The Beers criteria list skeletal muscle relaxants (SMR) as inappropriate for individuals 65 years of age and older because of anticholinergic effects, sedation, and risk of falls/fractures. Patients 65 years of age and older presenting to U.S. primary care clinics for injury, prescribed an SMR, are at risk for these events. SMR prescribing patterns in older adults with injury have not been well studied at the population level. Using nationally representative data, the prevalence of older adults prescribed an SMR presenting to U...
September 2016: Consultant Pharmacist: the Journal of the American Society of Consultant Pharmacists
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