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Topic:Pharmacology

Pharmacology in horses involves the study and application of drugs and medications to diagnose, treat, and prevent diseases and conditions in equine species. This field encompasses the understanding of pharmacokinetics and pharmacodynamics specific to horses, including how drugs are absorbed, distributed, metabolized, and excreted by the equine body. Commonly studied pharmacological agents in horses include non-steroidal anti-inflammatory drugs (NSAIDs), antibiotics, sedatives, and anthelmintics. Research in equine pharmacology focuses on determining appropriate dosages, understanding drug interactions, and minimizing adverse effects. This page compiles peer-reviewed research studies and scholarly articles that investigate the efficacy, safety, and regulatory aspects of pharmacological interventions in equine veterinary practice.
Cardiopulmonary effects and anaesthesia recovery quality in horses anaesthetized with isoflurane and low-dose S-ketamine or medetomidine infusions.
Veterinary anaesthesia and analgesia    February 25, 2016   Volume 43, Issue 6 623-634 doi: 10.1111/vaa.12359
Menzies MP, Ringer SK, Conrot A, Theurillat R, Kluge K, Kutter AP, Jackson M, Thormann W, Bettschart-Wolfensberger R.To evaluate cardiopulmonary effects and anaesthesia recovery quality in horses anaesthetized with isoflurane receiving medetomidine or S-ketamine infusions. Methods: Randomized, blinded, prospective clinical trial. Methods: Fifty horses undergoing elective surgery. Methods: After acepromazine and flunixin meglumine premedication, horses received medetomidine (7 μg kg-1 ) intravenously (IV). Anaesthesia was induced with midazolam and racemic ketamine (Med treatment group; 2.2 mg kg-1 ; n = 25) or S-ketamine (S-ket treatment group; 1.1 mg kg-1 ; n = 25) IV and maintained with isoflura...
Continuous positive airway pressure (CPAP) decreases pulmonary shunt in anaesthetized horses.
Veterinary anaesthesia and analgesia    February 24, 2016   Volume 43, Issue 6 611-622 doi: 10.1111/vaa.12357
Mosing M, MacFarlane P, Bardell D, Lüthi L, Cripps PJ, Bettschart-Wolfensberger R.To evaluate the effects of continuous positive airway pressure (CPAP) on intrapulmonary shunt, cardiac output and oxygen delivery in horses subjected to a 6 hour period of general anaesthesia. Methods: Randomized, experimental, crossover study. Methods: Ten healthy adult horses. Methods: Following medetomidine, diazepam and ketamine administration, orotracheal intubation was performed and horses positioned in dorsal recumbency. Anaesthesia was maintained with isoflurane carried in an oxygen and air mix (FiO 0.5) combined with a medetomidine infusion. Horses were anaesthetized twice and either...
Crystal structure of equine serum albumin in complex with cetirizine reveals a novel drug binding site.
Molecular immunology    February 17, 2016   Volume 71 143-151 doi: 10.1016/j.molimm.2016.02.003
Handing KB, Shabalin IG, Szlachta K, Majorek KA, Minor W.Serum albumin (SA) is the main transporter of drugs in mammalian blood plasma. Here, we report the first crystal structure of equine serum albumin (ESA) in complex with antihistamine drug cetirizine at a resolution of 2.1Å. Cetirizine is bound in two sites--a novel drug binding site (CBS1) and the fatty acid binding site 6 (CBS2). Both sites differ from those that have been proposed in multiple reports based on equilibrium dialysis and fluorescence studies for mammalian albumins as cetirizine binding sites. We show that the residues forming the binding pockets in ESA are highly conserved in h...
Effects of maternal dexamethasone treatment on pancreatic β cell function in the pregnant mare and post natal foal.
Equine veterinary journal    February 15, 2016   Volume 49, Issue 1 99-106 doi: 10.1111/evj.12560
Valenzuela OA, Jellyman JK, Allen VL, Holdstock NB, Fowden AL.Synthetic glucocorticoids are used to treat inflammatory conditions in horses. In other pregnant animals, glucocorticoids are given to stimulate fetal maturation with long-term metabolic consequences for the offspring if given preterm. However, their metabolic effects during equine pregnancy remain unknown. Objective: Thus, this study investigated the metabolic effects of dexamethasone administration on pregnant pony mares and their foals after birth. Methods: Experimental study. Methods: A total of 3 doses of dexamethasone (200 μg/kg bwt i.m.) were given to 6 pony mares at 48 h intervals beg...
Differential expression of β-tubulin isotypes in different life stages of Parascaris spp after exposure to thiabendazole.
Molecular and biochemical parasitology    February 12, 2016   Volume 205, Issue 1-2 22-28 doi: 10.1016/j.molbiopara.2016.02.004
Tydén E, Skarin M, Andersson-Franko M, Sjöblom M, Höglund J.Anthelmintic resistance (AR) to macrocyclic lactones (ML) has been described in Parascaris of horses world-wide. In contrast, benzimidazoles (BZ) are still effective, although reduced efficacy to this drug class was recently reported. The mode of action of BZ is binding to β-tubulin, which prevents polymerisation of microtubules. In this study, β-tubulin gene expression of isotypes 1 and 2 was investigated at seven time points (0, 6, 24, 72, 96 and 120 h) during embryogenesis and in adult worms. In addition, an in ovo larval developmental test was developed to study β-tubulin gene expressio...
Comparison of alfaxalone, ketamine and thiopental for anaesthetic induction and recovery in Thoroughbred horses premedicated with medetomidine and midazolam.
Equine veterinary journal    February 6, 2016   Volume 49, Issue 1 94-98 doi: 10.1111/evj.12548
Wakuno A, Aoki M, Kushiro A, Mae N, Kodaira K, Maeda T, Yamazaki Y, Ohta M.There is limited information on clinical use of the new injectable anaesthetic agent alfaxalone in Thoroughbred horses. Objective: To compare anaesthetic induction and recovery characteristics and cardiopulmonary responses between alfaxalone, ketamine and thiopental in Thoroughbred horses premedicated with medetomidine and midazolam. Methods: Randomised blinded experimental cross-over study. Methods: Six Thoroughbred horses were anaesthetised 3 times with alfaxalone 1 mg/kg bwt, ketamine 2.5 mg/kg bwt or thiopental 4 mg/kg bwt after premedication with medetomidine 6 μg/kg bwt and midazola...
Cardiovascular, respiratory and metabolic responses to apnea induced by atlanto-occipital intrathecal lidocaine injection in anesthetized horses.
Veterinary anaesthesia and analgesia    February 5, 2016   Volume 43, Issue 6 590-598 doi: 10.1111/vaa.12344
Guedes A, Aleman M, Davis E, Tearney C.To determine physiologic responses to apnea-induced severe hypoxemia in anesthetized horses. Methods: Prospective experimental study. Methods: Six university-owned horses with a median (range) body weight of 500 (220-510) kg and aged 13.5 (0.8-24.0) years scheduled for euthanasia. Methods: Xylazine-midazolam-ketamine-anesthetized horses breathing room air spontaneously were instrumented with a facial artery catheter for pressure measurement and blood sampling, and were made apneic with atlanto-occipital intrathecal lidocaine (4 mg kg ). Cardiopulmonary, biochemical and hematologic variable...
Extracellular calcium regulates protein tyrosine phosphorylation through calcium-sensing receptor (CaSR) in stallion sperm.
Molecular reproduction and development    February 3, 2016   Volume 83, Issue 3 236-245 doi: 10.1002/mrd.22615
Macías-García B, Rocha A, González-Fernández L.Protein tyrosine phosphorylation (PY), a hallmark of sperm capacitation, is inhibited by extracellular calcium in stallion sperm. The objective of this study was to determine the presence and influence of the calcium-sensing receptor (CaSR) in this phenomenon. First, the presence of the CaSR was demonstrated in stallion sperm. We then tested its function in these gametes using its inhibitor NPS2143 or its agonist AC34356. Sperm were capacitated for 4 hr in modified Whitten's medium with 25 mM bicarbonate plus NPS2143 and 2.4 mM calcium or AC34356 alone, followed by analysis of PY. Inhibi...
Quantification of horse plasma proteins altered by xylazine using the fluorogenic derivatization-liquid chromatography-tandem mass spectrometry.
Journal of equine science    February 3, 2016   Volume 26, Issue 4 141-146 doi: 10.1294/jes.26.141
Mori M, Ichibangase T, Yamashita S, Kijima-Suda I, Kawahara M, Imai K.In the doping tests currently used in horse racing, prohibited substances or their metabolites are usually directly detected in urine or blood samples. However, despite their lasting pharmaceutical effects, some prohibited substances are rapidly eliminated from horse urine and blood, making them difficult to detect. Therefore, new indirect biomarkers for doping, such as plasma proteins that are increased by the prohibited substances, have recently attracted much attention. Here, a fluorogenic derivatization-liquid chromatography-tandem mass spectrometry (FD-LC-MS/MS) method was adopted for hor...
The effect of isosorbide dinitrate on uterine and ovarian blood flow in cycling and early pregnant mares: A pilot study.
Theriogenology    January 14, 2016   Volume 85, Issue 9 1562-1567 doi: 10.1016/j.theriogenology.2016.01.009
Zoller D, Lüttgenau J, Steffen S, Bollwein H.Poor uterine perfusion has been proposed as a cause of infertility in mares. The objective of this study was to investigate the effect of isosorbide dinitrate (ISDN), a nitric oxide donor, on uterine and ovarian blood flow resistance during diestrus and early pregnancy in mares. Six Trotter mares, aged 7 to 14 years, were examined daily during the first 11 days of three diestrous periods, and five of those mares were also examined during the first 11 days of two pregnancies. Six mares randomly received a placebo, a low dose (30 mg, ISDN30), or a high dose of ISDN (60 mg, ISDN60) through t...
Regional heterogeneity in the reactivity of equine small pulmonary blood vessels.
Journal of applied physiology (Bethesda, Md. : 1985)    January 14, 2016   Volume 120, Issue 6 599-607 doi: 10.1152/japplphysiol.00975.2015
Stack A, Derksen FJ, Williams KJ, Robinson NE, Jackson WF.Regional differences in large equine pulmonary artery reactivity exist. It is not known if this heterogeneity extends into small vessels. The hypothesis that there is regional heterogeneity in small pulmonary artery and vein reactivity to sympathomimetics (phenylephrine and isoproterenol) and a parasympathomimetic (methacholine) was tested using wire myography on small vessels from caudodorsal (CD) and cranioventral (CV) lung of 12 horses [9 mares, 3 geldings, 8.67 ± 0.81 (age ± SE) yr, of various breeds that had never raced]. To study relaxation, vessels were precontracted with U46619 (10(-...
P2Y(1) receptors mediate purinergic relaxation in the equine pelvic flexure.
Veterinary journal (London, England : 1997)    January 8, 2016   Volume 209 74-81 doi: 10.1016/j.tvjl.2016.01.002
Mas M, Mañé N, Fernández F, Gallego D, Pumarola M, Jiménez M.In the equine large intestine, the knowledge of the basic mechanisms underlying motility function is crucial to properly treat motility disorders. P2Y1 receptors are responsible for mediating purinergic colonic relaxation in several species. In vitro experimental studies of the circular muscle from the equine pelvic flexure (n = 6) were performed to characterize inhibitory and excitatory neuromuscular transmission. Electrophysiological studies showed that electrical field stimulation (EFS) evoked biphasic inhibitory junction potentials (IJPs) in smooth muscle cells: a fast IJP (IJPf) follo...
The use of dexmedetomidine continuous rate infusion for horses undergoing transvenous electrical cardioversion–A case series.
The Canadian veterinary journal = La revue veterinaire canadienne    January 8, 2016   Volume 57, Issue 1 70-75 
Marly-Voquer C, Schwarzwald CC, Bettschart-Wolfensberger R.Five horses were presented for treatment of atrial fibrillation by transvenous electrical cardioversion (TVEC). A dexmedetomidine infusion was administered for sedation during positioning of the cardioversion catheters, and continued during general anesthesia. Shocks were applied until return to sinus rhythm. Dexmedetomidine infusion provided excellent conditions for TVEC catheter placement and procedure. Utilisation d’une perfusion continue de dexmedetomidine lors de cardioversion électrique transveineuse chez le cheval: une série de cas. Cinq chevaux présentant une fibrillation atriale ...
Aptamer based peptide enrichment for quantitative analysis of gonadotropin-releasing hormone by LC-MS/MS.
Talanta    January 7, 2016   Volume 150 671-680 doi: 10.1016/j.talanta.2016.01.006
Richards SL, Cawley AT, Cavicchioli R, Suann CJ, Pickford R, Raftery MJ.Over recent years threats to racing have expanded to include naturally occurring biological molecules, such as peptides and proteins, and their synthetic analogues. Traditionally, antibodies have been used to enable detection of these compounds as they allow purification and concentration of the analyte of interest. The rapid expansion of peptide-based therapeutics necessitates a similarly rapid development of suitable antibodies or other means of enrichment. Potential alternative enrichment strategies include the use of aptamers, which offer the significant advantage of chemical synthesis onc...
In vitro anticancer activity of Betulinic acid and derivatives thereof on equine melanoma cell lines from grey horses and in vivo safety assessment of the compound NVX-207 in two horses.
Chemico-biological interactions    January 7, 2016   Volume 246 20-29 doi: 10.1016/j.cbi.2016.01.002
Liebscher G, Vanchangiri K, Mueller T, Feige K, Cavalleri JM, Paschke R.Betulinic acid, a pentacyclic triterpene, and its derivatives are promising compounds for cancer treatment in humans. Melanoma is not only a problem for humans but also for grey horses as they have a high potential of developing melanoma lesions coupled to the mutation causing their phenotype. Current chemotherapeutic treatment carries the risk of adverse health effects for the horse owner or the treating veterinarian by exposure to antineoplastic compounds. Most treatments have low prospects for systemic tumor regression. Thus, a new therapy is needed. In this in vitro study, Betulinic acid a...
The Effect of Intravenous Regional Perfusion of the Distal Limb With Amikacin Sulfate on Wounds Healing by Second Intention in Horses.
Veterinary surgery : VS    January 6, 2016   Volume 45, Issue 1 125-132 doi: 10.1111/vsu.12435
Edwards-Milewski ML, Morello SL, Zhao Q, Mattan-Bell C.To compare the gross and histological effects of intravenous regional limb perfusion (IVRLP) using amikacin sulfate on second intention healing of distal limb wounds in adult horses with healing in untreated wounds. Methods: In vivo experimental study. Methods: Adult horses (n = 7). Methods: Two full thickness wounds (2.5 × 2.5 cm) were created aseptically on the dorsal aspect of each metacarpus and maintained under sterile bandages. One forelimb was randomly selected from each horse for IVRLP on days 2, 3, and 4 post-wounding. Sequential biopsies were taken from 1 wound on each limb to evalu...
Qualitative and Quantitative Characteristics of the Electroencephalogram in Normal Horses during Administration of Inhaled Anesthesia.
Journal of veterinary internal medicine    December 30, 2015   Volume 30, Issue 1 289-303 doi: 10.1111/jvim.13813
Williams DC, Brosnan RJ, Fletcher DJ, Aleman M, Holliday TA, Tharp B, Kass PH, LeCouteur RA, Steffey EP.The effects of anesthesia on the equine electroencephalogram (EEG) after administration of various drugs for sedation, induction, and maintenance are known, but not that the effect of inhaled anesthetics alone for EEG recording. Objective: To determine the effects of isoflurane and halothane, administered as single agents at multiple levels, on the EEG and quantitative EEG (qEEG) of normal horses. Methods: Six healthy horses. Methods: Prospective study. Digital EEG with video and quantitative EEG (qEEG) were recorded after the administration of one of the 2 anesthetics, isoflurane or halothane...
In vitro growth inhibitory efficacy of some target specific novel drug molecules against Theileria equi.
Veterinary parasitology    December 29, 2015   Volume 217 1-6 doi: 10.1016/j.vetpar.2015.12.024
Gopalakrishnan A, Maji C, Dahiya RK, Suthar A, Kumar R, Gupta AK, Dimri U, Kumar S.The in vitro growth inhibitory efficacies of five drug molecules against Theileria equi were evaluated in in vitro cultured parasites. A continuous microaerophilic stationary-phase culture (MASP) system was established for propagation of T. equi parasites. This in vitro culture system was used to assess the growth inhibitory effect of harmaline hydrochloride dihydrate (HHD), hexadecyltrimethylammonium bromide (HDTAB), hesparidin methyl chalcone (HMC), andrographolide and imidocarb dipropionate against T. equi. The 50% inhibitory concentration value of HHD, HDTAB, HMC, and imidocarb dipropionat...
Use of Liposomal Gentamicin for Treatment of 5 Foals with Experimentally Induced Rhodococcus equi Pneumonia.
Journal of veterinary internal medicine    December 22, 2015   Volume 30, Issue 1 322-325 doi: 10.1111/jvim.13810
Cohen ND, Giguère S, Burton AJ, Rocha JN, Berghaus LJ, Brake CN, Bordin AI, Coleman MC.Adverse effects of, and bacterial resistance to, macrolides used to treat Rhodococcus equi infections have prompted search for clinically effective alternative antimicrobials. Liposomal gentamicin (LG) is effective against R. equi in vitro and decreases tissue concentrations of R. equi in experimentally infected mice. Effectiveness of LG treatment of foals with R. equi pneumonia, however, has not been described. Objective: Liposomal gentamicin is safe and effective for treating foals with R. equi pneumonia. Methods: Ten foals with experimentally induced R. equi pneumonia. Methods: Pilot treatm...
Evaluation of coagulation via thromboelastography in healthy horses administered dexamethasone.
The Canadian veterinary journal = La revue veterinaire canadienne    December 18, 2015   Volume 56, Issue 12 1271-1274 
Woodman J, Wagg CR, Boysen SR, Leguillette R, Mizen K, Roy MF.Dexamethasone was administered to healthy horses daily for 7 days. Blood samples were collected at 3 time points from both treatment and non-treatment groups, and analyzed via thromboelastography (TEG). There were no significant differences in TEG parameters between treated and untreated horses, or within treatment groups over time. La dexaméthasone a été administrée à des chevaux en santé pendant 7 jours. Des échantillons de sang ont été prélevés à trois moments auprès des groupes de traitement et des groupes sans traitement et ensuite analysés par thrombo-élastographie (TEG)....
Towards the elimination of excessive cobalt supplementation in racing horses: A pharmacological review.
Research in veterinary science    December 17, 2015   Volume 104 106-112 doi: 10.1016/j.rvsc.2015.12.007
Kinobe RT.Cobalt is an essential trace element for many vital physiological functions. Cobalt is also known to stabilise hypoxia-inducible transcription factors leading to increased expression of erythropoietin which activates production of red blood cells. This implies that cobalt can be used to enhance aerobic performance in racing horses. If this becomes a pervasive practice, the welfare of racing animals would be at risk because cobalt is associated with cardiovascular, haematological, thyroid gland and reproductive toxicity as observed in laboratory animals and humans. It is expected that similar e...
Effect of firocoxib on cyclooxygenase 2, microsomal prostaglandin E2 synthase 1, and cytosolic phospholipase A2 gene expression in equine mononuclear cells.
American journal of veterinary research    December 1, 2015   Volume 76, Issue 12 1051-1057 doi: 10.2460/ajvr.76.12.1051
Barton MH, Darden JE, Clifton S, Vandenplas M.To validate primer sets for use in reverse transcription quantitative PCR assays to measure gene expression of cytosolic phospholipase A2 (cPLA2) and microsomal prostaglandin E2 synthase 1 (mPGES1) in equine mononuclear cells and determine the effects of firocoxib, a selective cyclooxygenase 2 (COX-2) inhibitor, on COX-2, cPLA2, and mPGES1 gene expression following incubation of mononuclear cells with lipopolysaccharide (LPS). Methods: 8 healthy adult horses. Methods: Peripheral blood mononuclear cells were isolated by density gradient centrifugation and incubated at 37°C with medium alone, f...
Anesthesia of the Equine Neonate in Health and Disease.
The Veterinary clinics of North America. Equine practice    November 28, 2015   Volume 31, Issue 3 567-585 doi: 10.1016/j.cveq.2015.09.002
Fischer B, Clark-Price S.Anesthetizing the neonatal foal presents significant challenges as a result of physiologic differences from the adult equine. This article gives the reader an overview of these differences and the impact they have on anesthetic drug selection, monitoring, and support of the equine neonate. Special emphasis is directed to the sick neonate and appropriate preparation and maintenance of anesthesia in the face of commonly presented disease conditions.
Initiative focuses on racing integrity. AAEP’s Prescription for Racing Reformto seek non-race day EIPH treatments.
Journal of the American Veterinary Medical Association    November 26, 2015   Volume 247, Issue 6 582-583 
Larkin M.No abstract available
Effect of Pre- and Postoperative Phenylbutazone and Morphine Administration on the Breathing Response to Skin Incision, Recovery Quality, Behavior, and Cardiorespiratory Variables in Horses Undergoing Fetlock Arthroscopy: A Pilot Study.
Frontiers in veterinary science    November 23, 2015   Volume 2 58 doi: 10.3389/fvets.2015.00058
Conde Ruiz C, Cruz Benedetti IC, Guillebert I, Portier KG.This prospective blinded randomized study aimed to determine whether the timing of morphine and phenylbutazone administration affects the breathing response to skin incision, recovery quality, behavior, and cardiorespiratory variables in horses undergoing fetlock arthroscopy. Ten Standardbred horses were premedicated with acepromazine (0.04 mg kg(-1) IM) and romifidine (0.04 mg kg(-1) IV). Anesthesia was induced with diazepam (0.05 mg kg(-1)) and ketamine (2.2 mg kg(-1)) IV at T0. Horses in group PRE (n = 5) received morphine (0.1 mg kg(-1)) and phenylbutazone (2.2 mg kg(-1)) I...
Effects of estradiol on uterine perfusion in anesthetized cyclic mares affected with uterine vascular elastosis.
Animal reproduction science    November 14, 2015   Volume 164 57-63 doi: 10.1016/j.anireprosci.2015.11.012
Esteller-Vico A, Liu IK, Vaughan B, Steffey EP, Brosnan RJ.Uterine vascular elastosis in mares is characterized by degeneration of uterine vasculature through thickening of the elastin layers. Factors commonly associated with this degeneration include age, parity, and chronic uterine endometritis. Affected mares have also been shown to exhibit decreases in uterine blood flow and perfusion of the uterus. Due to the increased thickness of the elastin layers, we hypothesize that vasodilatation of the uterine vasculature is also impaired. To test the functionality of these vessels, we evaluated the vasodilatory effects of estradiol on the uterine vascular...
Extrapyramidal system neurotoxicity: animal models.
Handbook of clinical neurology    November 14, 2015   Volume 131 207-223 doi: 10.1016/B978-0-444-62627-1.00012-3
Dorman D.The central nervous system's extrapyramidal system provides involuntary motor control to the muscles of the head, neck, and limbs. Toxicants that affect the extrapyramidal system are generally clinically characterized by impaired motor control, which is usually the result of basal ganglionic dysfunction. A variety of extrapyramidal syndromes are recognized in humans and include Parkinson's disease, secondary parkinsonism, other degenerative diseases of the basal ganglia, and clinical syndromes that result in dystonia, dyskinesia, essential tremor, and other forms of tremor and chorea. This cha...
Severe cutaneous vasculitis: an unusual complication of equine antithymocyte globulin treatment.
QJM : monthly journal of the Association of Physicians    November 11, 2015   Volume 109, Issue 6 411-412 doi: 10.1093/qjmed/hcv209
Vinod KV, Charles D, Hitha B, Radhakrishna P, Dutta TK.No abstract available
Tamoxifen as a new therapeutic tool for neutrophilic lung inflammation.
Respirology (Carlton, Vic.)    October 29, 2015   Volume 21, Issue 1 112-118 doi: 10.1111/resp.12664
Perez B, Henriquez C, Sarmiento J, Morales N, Folch H, Galesio JS, Uberti B, Morán G.Neutrophilic asthma is an important disease subgroup, including patients with severe phenotypes and erratic responses to standard treatments. Tamoxifen (TX), a selective estrogen receptor modulator (SERM) used as treatment of human breast cancer, has been shown to induce early apoptosis of equine blood and bronchoalveolar lavage fluid (BALF) neutrophils in vitro. Equine recurrent airway obstruction (RAO) is a naturally occurring neutrophilic condition, closely related with human asthma. Our purpose was to investigate the therapeutic potential of tamoxifen in horses with neutrophilic lung infla...
Erratum to: Sequence Elucidation of an Unknown Cyclic Peptide of High Doping Potential by ETD and CID Tandem Mass Spectrometry.
Journal of the American Society for Mass Spectrometry    October 29, 2015   Volume 27, Issue 2 370 doi: 10.1007/s13361-015-1294-8
Guan F, Uboh CE, Soma LR, Rudy J.No abstract available
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