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Drug Research

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https://www.readbyqxmd.com/read/30616250/2-benzylidene-1-indanone-analogues-as-dual-adenosine-a1-a2a-receptor-antagonists-for-the-potential-treatment-of-neurological-conditions
#1
HelenaDorathea Janse van Rensburg, LesetjaJ Legoabe, Gisella Terre'Blanche, MiethaM Van der Walt
Previous studies explored 2-benzylidine-1-tetralone derivatives as innovative adenosine A1 and A2A receptor antagonists for alternative non-dopaminergic treatment of Parkinson's disease. This study's aim is to investigate structurally related 2-benzylidene-1-indanones with substitutions on ring A and B as novel, potent and selective adenosine A1 and A2A receptor blockers. 2-Benzylidene-1-indanone derivatives were synthesised via acid catalysed aldol condensation reactions and evaluated via radioligand binding assays to ascertain structure activity relationships to govern A1 and A2A AR affinity...
January 7, 2019: Drug Research
https://www.readbyqxmd.com/read/30616249/study-of-dna-binding-activity-and-antibacterial-effect-of-escitalopram-oxalate-an-extensively-prescribed-antidepressant
#2
Reza Valipour, Mehmet Bertan Yilmaz, Ebrahim Valipour
Escitalopram oxalate (EO) is considered as one of the extensively prescribed antidepressant drug in Turkey and some other countries, therefore this research was aimed to study the interaction of the drug with DNA and study of the substance effect on bacterial growth. The absorption value of the drug solution at 238 nm was increased when DNA was added gradually to it and it showed hyperchromism effect. The value obtained for DNA binding constant (Kb) was 0.035  M -1 . When we added the CuCl2 2H2O to the mixture, any breakage was not shown in double strand DNA in comparison with control DNA...
January 7, 2019: Drug Research
https://www.readbyqxmd.com/read/30616248/effect-of-artemisia-aucheri-l-and-bupivacaine-encapsulated-nanoparticles-on-nociceptive-pain
#3
Mahmoud Reza Moradkhani, Arash Karimi
AIM: The purpose of this study was to evaluate the antinociceptive interaction between bupivacaine and Artemisia aucheri. L encapsulated nanoparticles. METHODS AND MATERIALS: The effect of bupivacaine and Artemisia aucheri.L alone, and their encapsulated co-administration was assessed using the 3% formalin test in rat. Increasing doses of bupivacaine (31.6, 100, 178, and 316 mg/kg) or Artemisia aucheri.L (5.6, 10, 17.8, and 31.6 mg/kg) were given i.p. 10 min before 3% formalin administration...
January 7, 2019: Drug Research
https://www.readbyqxmd.com/read/30609434/mechanistic-pathways-of-atp-sensitive-potassium-channels-referring-to-cardio-protective-effects-and-cellular-functions
#4
Vishal Kumar Vishwakarma, Prabhat Kumar Upadhyay, Hridaya Shanker Chaurasiya, Ritesh Kumar Srivasatav, Tarique Mahmood Ansari, Vivek Srivastava
A study of potassium channels correlates the fundamentals of mechanistic pathways and various physiological functions. The knowledge of these pathways provides the background, how to determine unit cell functions and to affect cardio protection. ATP sensitive potassium channels adjust excitability of membrane and functions as per metabolic status of cell. A lot of energy consumption primarily occurred in skeletal muscles which also express high number of potassium channels. The increase in calcium release and high heat production is occurred due to loss of potassium channels...
January 4, 2019: Drug Research
https://www.readbyqxmd.com/read/30609433/spinal-serotonin-and-5ht6-receptor-levels-during-development-of-neuropathy-and-influence-of-blockade-of-these-receptors-on-thermal-hyperalgesia-in-diabetic-mice
#5
Cagda Celik Sari, Ozgur Gunduz, Ahmet Ulugol
Little is known about the role of 5-HT6 receptors in the pathophysiology of neuropathic pain. The aim of this study is firstly, to investigate the influence of spinal and systemic 5-HT6 receptors on thermal hyperalgesia, one of the most significant symptoms of neuropathy occurring in diabetes; and secondly to determine spinal lumbar serotonin and 5-HT6 receptor levels during development of diabetic neuropathy in mice. Diabetes was produced in Balb/c mice with a single injection of streptozocin (150 mg/kg, i...
January 4, 2019: Drug Research
https://www.readbyqxmd.com/read/30572351/synthesis-and-anticonvulsant-studies-of-thiazolidinone-and-azetidinone-derivatives-from-indole-moiety
#6
Sachin Saini
2-Amino-5-(3'-indolomethylene)-1, 3 , 4 - oxadiazole (3): undergoes facile condensation with various aromatic aldehydes to gave 2-substitiuted arylidenylamino-5-(3'- indolomethylene) - 1, 3 , 4 - oxadiazole (4-8): . Cyclocondensation of (4-8): with thioglycolic acid and triethylamine yielded 3-[5'-(3"- indolomethylene)- 1', 3', 4'- oxadiazol-2'-yl]- 2- (substituted aryl)-4- thiazolidinones (9-13): and 1-[5'-(3"- indolomethylene) -1', 3', 4'- oxadiazol - 2'- yl ] -4-(substituted aryl) -2- azetidinones (14-18): ...
December 20, 2018: Drug Research
https://www.readbyqxmd.com/read/30572350/clinical-needs-as-a-starting-point-for-different-strategies-in-computational-drug-development
#7
César Portela
Traditionally, the first step in the development of drugs is the definition of the target, by choice of a biological structure involved in a disease or by recognition of a molecule with some degree of a biological activity that presents itself as druggable and endowed with therapeutic potential. The complexity of the pathophysiological mechanisms of disease and of the structures of the molecules involved creates several challenges in this drug discovery process. These difficulties also come from independent operation of the different parts involved in drug development, with little interaction between clinical practitioners, academic institutions and large pharmaceutical companies...
December 20, 2018: Drug Research
https://www.readbyqxmd.com/read/30536259/rp-hplc-uv-method-for-simultaneous-quantification-of-second-generation-non-steroidal-antiandrogens-along-with-their-active-metabolites-in-mice-plasma-application-to-a-pharmacokinetic-study
#8
Ashok Zakkula, Vinay Kiran, Umesh Todmal, Suresh P Sulochana, Ramesh Mullangi
A simple, specific and reproducible high-performance liquid chromatography (HPLC) assay method has been developed and validated for the quantitation of second generation antiandrogens and their active metabolites namely apalutamide, enzalutamide, N -desmethylenzalutamide (active metabolite of enzalutamide), darolutamide and ORM-15341 (active metabolite of darolutamide) in mice plasma. The method involves extraction of apalutamide, enzalutamide, N -desmethylenzalutamide, darolutamide and ORM-15341 along with internal standard (IS) from 100 µL mice plasma through a simple protein precipitation process...
December 10, 2018: Drug Research
https://www.readbyqxmd.com/read/30536258/jobelyn-attenuates-oxidative-stress-and-improves-memory-performance-in-mice-exposed-to-anoxic-stress
#9
Osarume Omorogbe
OBJECTIVE: Chronic stress impairs memory by damaging brain cells via induction of oxidative stress. Hence, the use of agents with antioxidant activity is being investigated as potential drugs against chronic stress-induced memory decline. This study evaluated the effect of Jobelyn® (JB), a potent antioxidant food supplement on memory deficit induced by anoxic stress in mice and on brain levels of biomarkers of oxidative stress. METHOD: Male mice were distributed into 6 groups (n=6): group 1 (non-stress control) and group 2 (stress control) were a given saline, groups 3-5 received JB (5, 10, 25 and 50 mg/kg) while group 6 had donepezil-DP (1 mg/kg)...
December 10, 2018: Drug Research
https://www.readbyqxmd.com/read/30536257/evaluation-of-isolated-vascular-response-to-5ht1a-5ht1b1d-5ht2a-receptors-agonist-antagonist-in-chronic-endotoxemic-rats
#10
Razieh Afshar Moghaddam, Farahnaz Jazaeri, Alireza Abdollahi, Razieh Mohammadjafari, Ahmad Reza Dehpour, Azam Bakhtiarian
The main vascular feature in endotoxemia is impaired contractile responses to vasoactive agents. We study the aortic response to 5HT11 A, 5HT1B1D and 5HT2A receptors agonist and antagonist in chronic endotoxemic rats. Intraperitoneal injection of 1 mg/kg lipopolysaccharide for 5 days induced chronic endotoxemia. Control rats received intraperitoneal injection of 1 ml/kg saline for 5 days. Rats divided into 3 groups. In first, DOI2 hydrochloride used as an agonist and sarpogrelate hydrochloride as an antagonist of 5HT2A receptor...
December 10, 2018: Drug Research
https://www.readbyqxmd.com/read/30517965/an-overview-on-genistein-and-its-various-formulations
#11
Neha Jaiswal, Juber Akhtar, Satya Prakash Singh, Farogh Ahsan
Genistein is the natural isoflavone and a phytoestrogen with a broad range of pharmacological properties, such as tyrosine and topoisomerase inhibition. It also induces apoptosis and cell proliferation inhibition, differentiates cancer cells. Added health benefits include the reduction of osteoporosis by suppressing osteoclasts and lymphocyte functions, decreased the risk of cardiovascular attacks and relieved postmenopausal problems. Genistein traditionally used in Chinese and Ayurvedic medicine and are found to be associated with lower risk of breast, prostate and lung cancer...
December 5, 2018: Drug Research
https://www.readbyqxmd.com/read/30463092/effect-of-flying-at-high-altitude-on-early-exposure-of-paracetamol-in-humans
#12
Nasir Idkaidek, Ahmad Al-Ghazawi
Pharmacokinetics of paracetamol (APAP) was studied on-board during an air flight and compared to those on ground after 500 mg oral dose in 20 healthy human volunteer in parallel design study. Saliva samples were obtained every 15 min up to 2 h after dosing. Pharmacokinetic parameters were calculated by non compartmental analysis and one compartment models using Winnonlin program V5.2. Results have showed that on-board to ground ratios for area under curves AUC0→1 , AUC0→2 , time to reach maximum saliva concentration Tmax , absorption rate constant Ka and maximum saliva concentration Cmax were 0...
November 21, 2018: Drug Research
https://www.readbyqxmd.com/read/30463091/safranal-attenuates-excitotoxin-induced-oxidative-oln-93-cells-injury
#13
Mohaddeseh Sadat Alavi, Sahar Fanoudi, Ameneh Veisi Fard, Mohammad Soukhtanloo, Mahmoud Hosseini, Hanif Barzegar, Hamid R Sadeghnia
OBJECTIVES: Researches have been shown that glutamic acid (GA) or quinolinic acid (QA) can play role in neuroinflammatory and demyelinating diseases including multiple sclerosis (MS), mainly via oligodendrocytes activation and extreme free radicals generation. Recent studies have demonstrated that safranal, an active constituent of Crocus sativus, has several pharmacological effects such as antioxidant, anti-inflammatory and neuroprotective properties. Since there is no data about the impact of safranal on MS, this study was designed to investigate the protective effect of safranal on OLN-93 oligodendrocytes injury induced by GA or QA...
November 21, 2018: Drug Research
https://www.readbyqxmd.com/read/30452078/investigating-intestinal-permeability-of-bortezomib-using-a-validated-hplc-uv-method
#14
Mohammad Mahmoudian, Parvin Zakeri-Milani, Hadi Valizadeh
Bortezomib (BTZ), as a proteasome inhibitor, has been used for treatment of patients with relapsed/refractory multiple myeloma and mantle cell lymphoma. BTZ is available for intravenous injection or subcutaneous administration. In this study, for evaluating the potential of BTZ oral delivery, intestinal permeability of BTZ was determined using in situ single-pass intestinal perfusion (SPIP) technique and the perfused solutions were analyzed using a validated HPLC-UV method. The chromatographic separation was performed using a C18 column via isocratic mode at a flow rate of 0...
November 16, 2018: Drug Research
https://www.readbyqxmd.com/read/30452077/in-vitro-anti-trypanosomal-activities-of-indanone-based-chalcones
#15
Richard M Beteck, Lesetje J Legoabe, Michelle Isaacs, Heinrich C Hoppe
Human African trypanosomiasis is a neglected infectious disease that affects mostly people living in the rural areas of Africa. Current treatment options are limited to just four drugs that have been in use of four to nine decades. The life-threatening toxic side-effects associated with the use of these drugs are disconcerting. Poor efficacy, low oral bioavailability, and high cost are other shortcomings of current HAT treatments. Evaluating the potentials of known hits for other therapeutic areas may be a fast and convenient method to discover new hit compounds against alternative targets...
November 16, 2018: Drug Research
https://www.readbyqxmd.com/read/30440077/are-grapes-able-to-mitigate-the-noxious-effects-induced-by-cadmium-exposure-in-different-tissues-and-or-organs-a-mini-review
#16
Bianca Andrade Handan, Caroline Margonato Cardoso, Luciana Pellegrini Pisani, Debora Estadella, Rosângela Soares Chriguer, Daniel Araki Ribeiro
Grapes are fruits that grow in clusters and can be crimson, black, dark blue, yellow, green, orange, and pink. Cadmium is a non-essential metal toxic to living organisms and the environment. Recently, health professionals, food scientists, and consumers have paid much attention to grapes for their health-promoting effects. To the best of our knowledge, there are no reviews describing the ability of grapes to mitigate the toxic effects induced by cadmium exposure in different tissues and/or organs. Herein, the aim of this review is to present the effects of grapes following cadmium exposure on the number of papers published in the scientific literature...
November 15, 2018: Drug Research
https://www.readbyqxmd.com/read/30577045/editorial
#17
(no author information available yet)
No abstract text is available yet for this article.
January 2019: Drug Research
https://www.readbyqxmd.com/read/30537766/acknowledgement-for-reviewers
#18
(no author information available yet)
No abstract text is available yet for this article.
December 2018: Drug Research
https://www.readbyqxmd.com/read/29966151/preparation-and-properties-of-5-fluorouracil-loaded-chitosan-microspheres-for-the-intranasal-administration
#19
Wanqing Li, Hongyuan Ba, Peng Huang, Aiping Zheng, Xi Yang
OBJECTIVE: To study the preparation technique of 5-fluorouracil and the release characteristic of 5-fluorouracil-loaded chitosan microspheres for the intranasal administration. METHODS: 5-fluorouracil-loaded chitosan microspheres were prepared by emulsion chemical cross-link technique. The orthogonal experimental design was used to optimize the preparation procedure. Dynamic dialysis method was applied to determine the release characteristic of microspheres in vitro and its influencing factors...
December 2018: Drug Research
https://www.readbyqxmd.com/read/29966150/effects-of-concomitant-administration-of-sodium-glucose-co-transporter-2-inhibitor-with-insulin-on-hemoglobin-a1c-body-mass-index-and-serum-lipid-profile-in-japanese-type-2-diabetic-patients
#20
Masataka Kusunoki, Yukie Natsume, Tetsuro Miyata, Kazuhiko Tsutsumi, Yoshiharu Oshida
In patients with type 2 diabetes mellitus who show suboptimal blood glucose control under insulin therapy alone, concomitant treatment with an additional hypoglycemic agent that differs in its mechanism of action from insulin may be considered. We conducted this clinical trial to explore whether further control of increased blood glucose level can be achieved with concomitant use of sodium glucose co-transporter 2 (SGLT2) inhibitor as concomitant with other hypoglycemic therapy, as compared to SGLT2 inhibitor monotherapy, in patients with type 2 diabetes mellitus showing decrease in blood glucose level but less than the effect of insulin monotherapy and there was no significant differences...
December 2018: Drug Research
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