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Fundamental & Clinical Pharmacology

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https://www.readbyqxmd.com/read/28815720/pharmacological-evidence-of-involvement-of-nitric-oxide-pathway-in-anti-pruritic-effects-of-sumatriptan-in-chloroquine-induced-scratching-in-mice
#1
Nazgol-Sadat Haddadi, Sattar Ostadhadi, Saeed Shakiba, Khashayar Afshari, Nastaran Rahimi, Arash Foroutan, Ahmad-Reza Dehpour
Chloroquine (CQ) induces histamine-independent itch in human and mice. We recently reported the role of intradermal nitric oxide (NO)/ cyclic guanosine monophosphate (cGMP) pathway in CQ-evoked scratching in mice. Chloroquine stimulates neuronal nitric oxide synthase (nNOS) activity to over-producing NO in the skin. Sumatriptan, a 5-hydroxytryptamine 1b/1d receptors (5-HTR1b/1d) agonist, is involved in pain and used to treat migraine and cluster headaches. According to previous studies, sumatriptan inhibits NOS activity...
August 16, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28802070/memantine-for-the-treatment-of-general-neuropathic-pain-a-narrative-review
#2
REVIEW
Gisèle Pickering, Véronique Morel
Neuropathic pain (NP) is difficult to treat and is associated with a decline in quality of life. NP aetiologies are numerous and a number of pathologies display neuropathic characteristics. Of the various N-Methyl-D-Aspartate antagonists that are alternatives to recommended in first-line NP treatment, memantine has the safest side-effect profile and has long been approved in Alzheimer's disease. The review covers memantine studies in post-herpetic neuralgia, diabetic pain, postoperative pain, complex regional pain syndrome, chronic phantom limb pain, opioid refractory pain, and fibromyalgia...
August 12, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28802065/quercetin-reverses-experimental-cirrhosis-by-immunomodulation-of-the-proinflammatory-and-profibrotic-processes
#3
Sael Casas-Grajales, Luis F Vázquez-Flores, Erika Ramos-Tovar, Erika Hernández-Aquino, Rosa E Flores-Beltrán, Carlos M Cerda-García-Rojas, Javier Camacho, Mineko Shibayama, Víctor Tsutsumi, Pablo Muriel
The ability of quercetin to reverse an established cirrhosis has not yet been investigated. Therefore, the aim of the present study was to examine the efficacy of this flavonoid in reversing experimental cirrhosis. Cirrhosis was induced by intraperitoneal administration of TAA (200 mg/kg of body weight) three times per week for 8 weeks or by intraperitoneal petrolatum-CCl4 (400 mg/kg of body weight) administration three times per week for 8 weeks. To determine the capacity of quercetin to prevent liver fibrosis, the flavonoid (50 mg/kg of body weight, p...
August 12, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28779530/pharmacology-and-drug-development-in-rare-diseases-the-attractiveness-and-expertise-of-the-french-medical-pharmacology
#4
Joëlle Micallef, Pierre Boutouyrie, Olivier Blin
Developing drugs for rare disease can be challenging due to specific rare disease characteristics. The French Medical Pharmacology is structured and positioned to play a major role in Orphan Drug Research and Development due to the required expertise concentrated into pharmacology departments, exclusively implemented within the French University Hospitals, public hospitals that are linked to a medical school (and often a pharmacy school) with numerous INSERM or CNRS labelled research units. In addition, these structures allow a close collaboration between researchers, academic institutions and biotech start-up (most of them being spin-off of the academic structures)...
August 5, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28767167/the-impact-of-age-and-sex-on-the-reporting-of-cough-and-angioedema-with-ras-inhibitors-a-case-non-case-study-in-vigibase
#5
Fawaz F Alharbi, Anzhelika A V Kholod, Patrick C Souverein, Ronald H Meyboom, Mark C H de Groot, Anthonius de Boer, Olaf H Klungel
The purpose of this study was to assess the impact of age and sex on the reporting of cough and angioedema related to renin angiotensin system (RAS) inhibitors. A case/non-case study was performed in VigiBase. Two case groups were identified, reports of cough and reports of angioedema and non-cases were all reports of all other adverse events. Logistic regression analysis was used to assess the association between reporting of cough and angioedema with each class of RAS inhibitors stratified by age/sex and to control for confounding...
August 2, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28755515/bufalin-a-bufanolide-steroid-from-the-parotoid-glands-of-the-chinese-toad-suppresses-herg-k-currents-expressed-in-hek293-cells
#6
Tao Song, Yuanyuan Zhang, Qiongtao Song, Xue Han, Shengjiang Guan, Xuan Zhang, Xi Chu, Fenghua Zhang, Jianping Zhang, Li Chu
In this study, we investigated the effect of bufalin on the human ether-à-go-go-related gene (hERG) K(+) channels using the perforated patch recording technique. We measured a half-maximal inhibitory concentration (IC50 ) of 24.83 μM and maximal inhibitory effect of 39.45 ± 1.14% with bufalin. These findings suggest that bufalin is a potent hERG K(+) channel blocker and may provide a new way for understanding Chan Su-induced arrhythmia. This article is protected by copyright. All rights reserved.
July 29, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28727906/potential-of-telmisartan-in-the-treatment-of-benign-prostatic-hyperplasia
#7
Ismail Ogunbayode Ishola, Charles C Anunobi, Kehinde Habeeb Tijani, Olasunmbo Afolayan, Victoria U Udokwu
Benign prostatic hyperplasia (BPH) is a common health problem in aging men. This study was carried out to investigate the protective effect of telmisartan on testosterone induced-BPH in rats. Fifty-four male Wistar rats (200 - 250g) were randomly divided into 9 groups (n =6) and orally treated for 28 consecutive days: group 1- vehicle normal, olive oil (10 ml/kg); group 2- BPH model control (10 ml/kg); groups 3-5 - telmisartan (5, 10 or 20 mg/kg, respectively); group 6- pioglitazone (20 mg/kg); group 7- celecoxib (20 mg/kg); group 8- combination of telmisartan (5 mg/kg) and pioglitazone (20 mg/kg); group 9- combination of telmisartan (5 mg/kg) and celecoxib (20 mg/kg)...
July 20, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28692163/pre-treatment-with-melatonin-protects-against-cyclophosphamide-induced-oxidative-stress-and-renal-damage-in-mice
#8
Mehdi Goudarzi, Mohammad Javad Khodayar, Seyed Mohammad Taghi Hosseini Tabatabaei, Habib Ghaznavi, Iman Fatemi, Saeed Mehrzadi
Cyclophosphamide (CP) is widely used in treatment of different cancers. Nephrotoxicity is one of the dose-limiting side effects of CP. This study was done to investigate the effect of melatonin (MEL) on CP-induced nephrotoxicity in mice. In this study, 50 Swiss albino mice (20-25 g) were randomly divided into five groups. Mice were pretreated with MEL intraperitoneally (i.p) in doses of 5, 10 and 20 mg/kg for 5 consecutive days and CP (200 mg/kg, i.p) was administrated on the 5(th) day 1 hour after the last dose of MEL...
July 10, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28677297/naloxone-prolongs-cutaneous-nociceptive-block-by-lidocaine-in-rats
#9
Yu-Wen Chen, Ja-Ping Shieh, Kuo-Sheng Liu, Jhi-Joung Wang, Ching-Hsia Hung
We aimed to investigate the local anesthetic properties of naloxone alone or as an adjunct for the local anesthetic lidocaine. After the block of the cutaneous trunci muscle reflex (CTMR) with drugs delivery by subcutaneous infiltration, cutaneous nociceptive block was tested on the ratsꞌ backs. We demonstrated that naloxone, as well as lidocaine elicited cutaneous analgesia dose-dependently. The relative potency in inducing cutaneous analgesia was lidocaine [22.6 (20.1 - 25.4) μmol/kg] > naloxone [43...
July 4, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28636803/atorvastatin-attenuates-testosterone-induced-benign-prostatic-hyperplasia-in-rats-role-of-peroxisome-proliferator-activated-receptor-%C3%AE-and-cyclo-oxygenase-2
#10
Ismail O Ishola, Habeeb K Tijani, Olufunke O Dosumu, Charles C Anunobi, Tolulope O Oshodi
Diabetes and obesity have been reported to alter sex steroid hormone metabolism. In this study, an attempt was made to investigate the protective effect of atorvastatin (ATR) in combination with celecoxib (CEL) or pioglitazone (PIO) on testosterone-induced BPH in rats. Male Wistar rats (200-250 g) were randomly divided into 9 groups (n=8) and orally treated as follows for 28 consecutive days; Group 1: vehicle (10 ml/kg), group 2: vehicle (10 ml/kg), groups 3 - 5: ATR (0.5, 2.5 and 5 mg/kg, respectively); group 6: CEL (20 mg/kg); Group 7: PIO (20 mg/kg); Groups 8-9: ATR 0...
June 21, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28622415/is-bisphenol-a-an-environmental-obesogen
#11
REVIEW
Samuel Legeay, Sébastien Faure
Bisphenol A (BPA) is an endocrine disruptor with an oestrogenic activity that is widely produced for the manufacture of polycarbonate plastic, epoxy resin, and thermal paper. Its ubiquitous presence in the environment contributes to broad and continuous human exposure, which has been associated with deleterious health effects. Despite numerous controversial discussions and a lack of consensus about BPA's safety, growing evidence indicates that BPA exposure positively correlates with an increased risk of developing obesity...
June 16, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28575541/trends-in-the-incidence-of-use-of-non-insulin-glucose-lowering-drugs-between-2006-and-2013-in-france
#12
Mickael Arnaud, Julien Bezin, Bernard Bégaud, Antoine Pariente, Francesco Salvo
This study aimed at describing trends in the incidence of use of non-insulin glucose-lowering drugs (NIGLDs) between 2006 and 2013 in France. Repeated cross-sectional studies on NIGLD new users were performed annually from 2006 to 2013 within the Echantillon Généraliste des Bénéficiaires (EGB) database, a 1/97(th) representative sample of the population covered by the French healthcare insurance system. NIGLD included metformin, sulfonylureas, α-glucosidase inhibitors, thiazolidinediones, dipeptidylpeptidase-4 (DPP-4) inhibitors, glinides and glucagon-like peptide-1 analogues...
June 2, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28544244/branched-chain-amino-acids-supplementation-modulates-tgf-%C3%AE-1-smad-signaling-pathway-and-interleukins-in-ccl4-induced-liver-fibrosis
#13
Naglaa F Khedr, Eman G Khedr
The alterations and low levels of circulating branched chain amino acids (BCAAs), leucine, isoleucine and valine, are associated with liver diseases. The study was designed to evaluate hepatoprotective effect of BCAAs on CCl4 -induced liver fibrosis and to investigate the molecular mechanisms underlying these effects in rats. Thirty male rats were divided into three groups. Control group (n=10), CCl4 group (n=10); rats were injected with CCl4 (1 mL/kg of 0.5:1 v/v injected i.p. twice weekly for 12 weeks). CCl4 +BCAAs group (n=10); rats were injected with similar doses of CCl4 and supplemented with a mixture of 600 mg/kg BCAAs (2: 1: 1...
May 23, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28543930/further-analysis-of-acute-antinociceptive-and-anti-inflammatory-actions-of-4-phenylselenyl-7-chloroquinoline-in-mice
#14
Vanessa D G Silva, Angélica S Reis, Mikaela Pinz, Caren A R da Fonseca, Luis Fernando B Duarte, Juliano A Roehrs, Diego Alves, Cristiane Luchese, Ethel A Wilhelm
A new quinoline containing selenium, 4-phenylselenyl-7-chloroquinoline (4-PSQ), was described and synthetized by our research group. Recently, we demonstrated the potential antinociceptive and anti-inflammatory of 4-PSQ. For this reason, the first objective of this study was to expand our previous findings by investigating the contribution of glutamatergic, serotonergic and nitrergic systems to the acute antinociceptive action of this compound. Pretreatment with 4-PSQ (0.01-25 mg/kg, p.o.) reduced the nociception induced by glutamate...
May 23, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28543864/modulation-of-heme-oxygenase-1-expression-and-activity-affects-streptozotocin-induced-diabetic-nephropathy-in-rats
#15
Marwa A M Ali, Gehan H Heeba, Azza A K El-Sheikh
Heme oxygenase (HO)-1 has exhibited nephro-protective actions in different animal models; however, its full mechanistic potential in diabetic nephropathy (DN) has not yet been elucidated. Hence, the present study has been undertaken by inducing DN in rats using streptozotocin (50mg/kg i.p.), with or without either HO-1 inducer; hemin (HM; 40 μmol/kg, s.c.), or HO-1 blocker; zinc protoporphyrin-IX (ZnPP; 50 μmol/kg, i.p.), for one month. Compared to control, rats with DN suffered from hyperglycemia and hyperlipidemia, with signs of renal damage, as assessed by distortion in renal histopathological architecture and kidney function...
May 23, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28675521/corrigendum
#16
(no author information available yet)
No abstract text is available yet for this article.
August 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28012206/uptake-and-efflux-kinetics-and-intracellular-activity-of-voriconazole-against-aspergillus-fumigatus-in-human-pulmonary-epithelial-cells-a-new-application-for-the-prophylaxis-and-early-treatment-of-invasive-pulmonary-aspergillosis
#17
Taotao Wang, Qianting Yang, Lu Chen, Ying Li, Ti Meng, Yan Wang, Tao Zhang, Jin'e Lei, Jianfeng Xing, Yalin Dong
Invasive pulmonary aspergillosis (IPA), most caused by Aspergillus fumigatus, is a serious life-threatening infection in immunocompromised patients. Voriconazole is used to prevent and treat IPA. However, little is known about the pharmacological characteristics of voriconazole in pulmonary epithelial cells, which are the target site for the prophylaxis and early treatment of IPA. The aim of the study was to evaluate the kinetics and activity of voriconazole against A. fumigatus in A549 cells. High-performance liquid chromatography/tandem mass spectrometry and time-kill method were used to study the cellular pharmacokinetic and pharmacodynamics of voriconazole...
June 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27891661/synergistic-effects-of-polydatin-and-vitamin-c-in-inhibiting-cardiotoxicity-induced-by-doxorubicin-in-rats
#18
Hui-Lin Wang, Xiao-Hua Cui, Hai-Lun Yu, Rong Wu, Xu Xu, Jian-Ping Gao
The purpose of this study was to assess the synergistic effect of polydatin and vitamin C on attenuating cardiotoxicity induced by doxorubicin (DOX) in rats. Polydatin could significantly increase the activity of superoxide dismutase (SOD) and the heart rate, attenuate myocardial pathological damage, decrease malondialdehyde (MDA) content, slightly increase arterial pressure and glutathione peroxidase (GSH-Px) activity, reduce intervals of QRS, QT, and ST, and lower free fatty acid (FFA) content. The combination of polydatin and vitamin C could significantly increase arterial pressure and heart rate, decrease QRS interval and slightly reduce ST and QT intervals, significantly attenuate myocardial pathological damage, increase the activities of GSH-Px,T-SOD, Na(+) K(+) -ATPase, and Ca(2+) Mg(2+) -ATPase, elevate phosphocreatine (PCr) and adenosine triphosphate (ATP) contents, slightly increase adenosine diphosphate (ADP) and total adenine nucleotide (TAN) contents and PCr/ATP, and significantly decrease the contents of MDA and FFA, when compared with those in the DOX group...
June 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27885727/growth-inhibitory-and-proapoptotic-effects-of-l-asparaginase-from-fusarium-culmorum-asp-87-on-human-leukemia-cells-jurkat
#19
Anil K Meghavarnam, Maryam Salah, Meenakshisundaram Sreepriya, Savitha Janakiraman
The objective of this study was to evaluate the anticancer properties of l-asparaginase purified from fungal isolate Fusarium culmorum ASP-87 against human T-cell leukemia cell line (Jurkat). The growth inhibitory and proapoptotic effects of purified l-asparaginase on Jurkat cell lines were investigated by determining its influence on cell viability, colony formation, DNA fragmentation, and cell cycle progression. The results revealed that purified l-asparaginase showed significant decrease in cell survival with IC50 value of 90 μg/mL (9 IU/mL)...
June 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28477356/epigallocatechin-3-gallate-ameliorates-intrahepatic-cholestasis-of-pregnancy-by-inhibiting-matrix-metalloproteinase-2-and-matrix-metalloproteinase-9
#20
Mei Zhang, Meimei Xu
Matrix metalloproteinase (MMP)-2 and matrix metalloproteinase-9 are involved in many illnesses affecting pregnant women, including intrahepatic cholestasis of pregnancy (ICP), a serious liver abnormality during pregnancy. Epigallocatechin-3-gallate (EGCG) has been widely reported to inhibit activities of MMP-2 and MMP-9. We aimed to investigate the role of EGCG in ameliorating ICP symptoms in a rat model. Using 17α-ethinylestradiol to induce ICP in pregnant rats, we investigated the efficacy of EGCG administration on ICP symptoms, including bile flow rate, total bile acids (TBA) and MMP-2 and MMP-9 activities...
May 5, 2017: Fundamental & Clinical Pharmacology
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