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Naunyn-Schmiedeberg's Archives of Pharmacology

Jonathan Palma, Madhusudhanan Narasimhan, Josée Guindon, Khalid Benamar
The growing therapeutic use (self-medication) of cannabinoids by HIV-1 infected people and the recent interest in the possible medicinal use of cannabinoids, particularly in pain management, create an urgent need to identify their potential interactions with HIV-1. The goal here is to determine any interaction between proteins of HIV-1 and the analgesic effectiveness of cannabinoid at supraspinal level. Young adult male rats (Sprague-Dawley) were stereotaxically pretreated with HIV-1 envelope glycoprotein 120 (gp120) into the periaqueductal gray (PAG) area, the primary control center of pain modulation...
July 15, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Ingo Staudacher, Claudius Illg, Sam Chai, Isabelle Deschenes, Sebastian Seehausen, Dominik Gramlich, Mara Elena Müller, Teresa Wieder, Ann-Kathrin Rahm, Christina Mayer, Patrick A Schweizer, Hugo A Katus, Dierk Thomas
K2P 17.1 (TASK-4, TALK-2) potassium channels are expressed in the heart and represent potential targets for pharmacological management of atrial and ventricular arrhythmias. Reduced K2P 17.1 expression was found in atria and ventricles of heart failure (HF) patients. Modulation of K2P 17.1 currents by antiarrhythmic compounds has not been comprehensively studied to date. The objective of this study was to investigate acute effects of clinically relevant antiarrhythmic drugs on human K2P 17.1 channels to provide a more complete picture of K2P 17...
July 14, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Mohaddeseh Ebrahimi-Ghiri, Mohammad Nasehi, Mohammad-Reza Zarrindast
The present study investigated the role of dopamine D2 receptors (D2Rs) of the dorsal hippocampus (DH) and the nucleus accumbens (NAc) and the effect of their dopaminergic activities on anxiety-like behavior and aversive learning using a test-retest elevated plus-maze (EPM) paradigm in male Wistar rats. Guide cannulae were implanted to allow microinjection of D2R agonist quinpirole or antagonist sulpiride. The pre-test intra-NAc microinjection of quinpirole (0.0625-0.25 μg/rat) or sulpiride (0.125-0.5 μg/rat) increased the percentage of time spent in the open arms (%OAT) of EPM, suggesting an anxiolytic-like effect...
July 13, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Pavitra Kumar, Harish A Kumar, Lakshmikirupa Sundaresan, Anuran Ghosh, Priyadarshan Kathirvel, Apurva Thilak, Yash T Katakia, Kavitha Sankaranarayanan, Suvro Chatterjee
Despite of medical disaster caused by thalidomide in 1960s, the drug came to clinical use again for the treatment of erythema nodosum leprosum (ENL) and multiple myeloma. Recently, a new generation of children affected by thalidomide intake by their mothers during pregnancy has been identified in Brazil. In the past few years, there is the great enhancement in our understanding of the molecular mechanisms and targets of thalidomide with the help of modern OMICS technologies. However, understanding of cardiac-specific anomalies in fetus due to thalidomide intake by the respective mother has not been explored fully...
July 7, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Parvin Zareie, Mahsa Gholami, Behnam Amirpour-Najafabadi, Sirvan Hosseini, Mehdi Sadegh
Learning and memory deficits appear in chronic diabetes and valproic acid has been proved to be beneficial in neurodegenerative diseases. Hence, the current study investigated the effectiveness of chronic valproate treatment for diabetes-induced memory impairment and increased levels of hippocampal apoptotic caspases. This study was conducted in adult male C57B15/J mice. Diabetes, which was induced by alloxan (150 mg/kg; i.p.), was confirmed when fasting blood sugar (FBS) was > 200 mg/dl. Sodium valproate (100 mg/kg; i...
July 4, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Kumiko Taguchi, Nanami Bessho, Mari Hida, Haruka Narimatsu, Takayuki Matsumoto, Tsuneo Kobayashi
Abnormal G protein-coupled receptor kinase 2 (GRK2) accumulation has a crucial role in the development of insulin resistance and diabetes. Although GRK2 siRNA transfection in the liver improves insulin resistance-related vascular complications, the effects of GRK2 siRNA in lipid metabolism and obesity remain unknown. To investigate how GRK2 siRNA affects obesity, ob/ob mice were transfected with GRK2 siRNA, mainly in the liver, by using a hydrodynamic-based procedure. Epididymal fat, glucose, triglyceride, non-esterified fatty acid (NEFA), and alanine transaminase activity were higher in the control siRNA-transfected ob/ob mice than in the control siRNA-transfected Lean mice, but these parameters were reduced by GRK2 siRNA transfection into the ob/ob mice...
June 26, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Matthias Irmen, Janine Holze, Theresa Bödefeld, Christian Tränkle
Firstly, it was determined whether methanthelinium bromide (MB) binds to human M1 -M5 (hM1 -hM5 ) muscarinic acetylcholine receptors in comparison to the classical muscarinic antagonist N-methylscopolamine (NMS). [3 H]NMS dissociation binding experiments revealed an allosteric retardation of dissociation at 100 μM of MB ranging from none in hM3 to 4.6-fold in hM2 receptors. Accordingly, global non-linear regression analysis of equilibrium inhibition binding curves between [3 H]NMS (0.2 and 2.0 nM) and MB was applied and compared using either an allosteric or a competitive model...
June 24, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Sana Khalid, Nabeel Afzal, Junaid Ali Khan, Zulfia Hussain, Anas Sarwar Qureshi, Hafeez Anwar, Yasir Jamil
The upsurge in copper oxide nanoparticle (CuONP) applications in various fields triggers hazardous effects on health. Resveratrol, a polyphenol found in plants of stilbene class, has been reported to decrease oxidative stress. The current study investigated the protective effect of resveratrol (RVT) against CuONP-induced hepatotoxicity and nephrotoxicity in male Wistar rats. CuONPs were prepared by precipitation method and characterized by X-ray diffraction (XRD) technique and scanning electron microscopy (SEM)...
June 23, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Lucie Navrátilová, Lenka Applová, Pavel Horký, Přemysl Mladěnka, Petr Pávek, František Trejtnar
Membrane organic anion-transporting polypeptides (OATPs) are responsible for the drug transmembrane transport within the human body. The function of OATP2B1 transporter can be inhibited by various natural compounds. Despite increased research interest in soya as a part of human diet, the effect of its active components to interact with hOATP2B1 has not been elucidated in a complex extent. This in vitro study examined the inhibitory effect of main soy isoflavones (daidzin, daidzein, genistin, genistein, glycitin, glycitein, biochanin A, formononetin) and their metabolites formed in vivo (S-equol, O-desmethylangolensin) towards human OATP2B1 transporter...
June 22, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Marjan Amiri, Martin C Michel
The impact factor is a frequently applied tool in research output analytics. Based on five consecutive publication years each of five pharmacology journals, we have analyzed to which extent review articles yield more impact factor-relevant citations than original articles. Our analysis shows that review articles are quoted about twice as often as original articles published in the same year in the same journal. We conclude that inclusion of review articles does not substantially affect the impact factor of a journal unless they account for considerably more than 10% of all published articles...
June 21, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Shigeyuki Yamashita, Tokiko Suzuki, Keisuke Iguchi, Takuya Sakamoto, Kengo Tomita, Hiroki Yokoo, Mari Sakai, Hiroki Misawa, Kohshi Hattori, Toshi Nagata, Yasuhide Watanabe, Naoyuki Matsuda, Naoki Yoshimura, Yuichi Hattori
Levosimendan and milrinone may be used in place of dobutamine to increase cardiac output in septic patients with a low cardiac output due to impaired cardiac function. The effects of the two inotropic agents on cardiac inflammation and left ventricular (LV) performance were examined in mice with cecal ligation and puncture (CLP)-induced sepsis. CLP mice displayed significant cardiac inflammation, as indicated by highly increased pro-inflammatory cytokines and neutrophil infiltration in myocardial tissues. When continuously given, levosimendan prevented but milrinone exaggerated cardiac inflammation, but they significantly reduced the elevations in plasma cardiac troponin-I and heart-type fatty acid-binding protein, clinical markers of cardiac injury...
June 20, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Maha Mohammed Abdel-Fattah, Basim Anwar Shehata Messiha, Ahmed Mohamed Mansour
The brain renin-angiotensin system (RAS) is considered a crucial regulator for physiological homeostasis and disease progression. We evaluated the protective effects of the angiotensin receptor blocker (ARB) telmisartan and the angiotensin-converting enzyme 2 (ACE2) activator xanthenone on experimental cerebral ischemia/reperfusion (I/R) injury. Rats were divided into a sham control, a cerebral I/R control, a standard treatment (nimodipine, 10 mg/kg/day, 15 days, p.o.), three telmisartan treatments (1, 3, and 10 mg/kg/day, 15 days, p...
June 17, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Manish Kumar, Nitin Bansal
Ellagic acid (EGA)-enriched dietary supplements are widely acclaimed, owing to its versatile bioactivities. Previously, we reported that chronic administration of EGA prevented the impairment of cognitive abilities in rats using the intracerebroventricular-administered streptozotocin (STZ-ICV) model of Alzheimer's disease. Impairment of phosphoinositide 3 (PI3)-kinase-regulated endothelial nitric oxide synthase (eNOS) activity by central administration of STZ in rodents instigates dementia. The aim of the present study was to delineate the role of PI3-kinase-eNOS activity in the prevention of STZ-ICV-induced memory dysfunctions by EGA...
June 15, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Nicolas Keller, Stefan Dhein, Joachim Neumann, Ulrich Gergs
Cisapride and prucalopride act as 5-HT4 receptor agonists. As a part of our ongoing effort to study the utility of a transgenic (TG) mouse model overexpressing cardiac 5-HT4 receptors, we assessed the extent to which we could recapitulate cisapride and prucalopride agonists. Contractile studies were performed using isolated left and right atrial preparations of TG mice showing cardiac-specific human 5-HT4a receptor expression and those of their wild-type (WT) littermates. 5-Hydroxytryptamine (5-HT), cisapride, and prucalopride exerted concentration-dependent positive inotropic effects in the left atrial preparations of TG mice...
June 9, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Tulsankar Sachin Laxman, Santosh Kumar Puttrevu, Rajesh Pradhan, Anjali Mishra, Sarvesh Verma, Yashpal S Chhonker, Swarnim Srivastava, Suriya P Singh, Koneni V Sashidhara, Rabi Sankar Bhatta
The present study was designed to investigate the oral bioavailability, metabolism, tissue disposition and excretion of 16α-hydroxycleroda-3, 13(14) Z -dien-15, 16-olide (4655K-09), a novel HMG-CoA reductase inhibitor in male Sprague Dawley (SD) rats. Tissue distribution, oral bioavailability and excretion studies of 4655K-09 were carried out in male SD rats through oral administration at active dose of 25 mg/kg. In vitro metabolism studies were carried out in different rat tissues S9 fractions to evaluate primary organs responsible for conversion of parent 4655K-09 to its major active metabolite K-9T...
June 6, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Mohammad I Saleh, Nagham N Hindi
Neutropenia is a hematologic disorder commonly reported in patients with chronic hepatitis C viral (HCV) infection. The objective of the present analysis is to describe the change in neutrophil count resulting from peglated interferon alpha 2-a (PEG-IFN α-2a) therapy in HCV-infected patients. A population pharmacodynamic model will be developed. We also plan to identify patient characteristics that contribute to the development of PEG-IFN α-2a-induced neutropenia in hepatitis C patients. A population pharmacodynamic modeling approach was applied to a cohort of patients (n = 292) with chronic HCV infection...
June 5, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Ahmed A Abdelsameea, Soad L Kabil
Peripheral nervous system neurotoxicity is the most problematic complication of cisplatin treatment. In this study, we have addressed the possible neuroprotective effect of canagliflozin on cisplatin-induced peripheral neurotoxicity in rats. Rats were randomly allocated into the following: control (vehicle) group, received hydhroxypropyl methyl cellulose; cisplatin group, injected cisplatin 2 mg/kg intraperitoneal, twice a week for 5 consecutive weeks; canagliflozin-cisplatin of received canagliflozin, 10 mg/kg/day by gavage and cisplatin in the same schedule like cisplatin group...
June 3, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Gaaminepreet Singh, Pawan Krishan
Early renal morphological alterations including glomerular hypertrophy and mesangial expansion occur in diabetic kidney disease and correlate with various clinical manifestations of diabetes. The present study was designed to investigate the influence of pharmacological modulation of HIF-1α (hypoxia inducible factor-1 alpha) protein levels, on these glomerular changes in rodent model of type 1 diabetes. Male wistar rats were made diabetic (Streptozotocin 45 mg/kg; i.p.) and afterwards treated with HIF activator cobalt chloride for 4 weeks...
June 2, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Filiz Mercantepe, Tolga Mercantepe, Atilla Topcu, Adnan Yılmaz, Levent Tumkaya
Despite the enormous advances made in the field of oncology, no solution to the side effect of nephrotoxicity caused by cisplatin used as an antineoplastic agent for approximately 40 years has yet been discovered. This study investigated the effects of cisplatin on the kidney, the damage mechanism involved, and the potential capacity of agents such as amifostine, curcumin, and melatonin to elicit a future therapeutic protocol in cisplatin-induced nephrotoxicity at the ultrastructural and molecular levels. Our study consisted of five groups: control (saline solution only; group 1), cisplatin (cisplatin only; group 2), cisplatin + amifostine (group 3), cisplatin + curcumin (group 4), and cisplatin + melatonin (group 5)...
June 2, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Nadia M J Rupniak, Mary Katofiasc, Edward C Burgard, Karl B Thor
The effects of the tachykinin NK2 receptor agonist LMN-NKA ([Lys5 ,MeLeu9 ,Nle10 ]-NKA(4-10) ) on colorectal and arterial blood pressure were examined in anesthetized macaques. Intravenous (IV) administration of 1-100 μg/kg caused dose-related increases in colorectal pressure up to 120 mmHg above baseline, and area under the curve (AUC) up to 24,987 mmHg*s. This was accompanied at all doses by transient hypotension, with up to 26% reduction in mean arterial pressure (MAP) from baseline. Hypotension, but not the increase in colorectal pressure, was inhibited by a 10-min pretreatment with the NK1 receptor antagonist CP-99,994...
June 1, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
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