Benzimidazoles

Publication Title: 
Methods and Findings in Experimental and Clinical Pharmacology

The general pharmacological profile and effects of E-4716 on the CNS have been investigated in comparison with other histamine receptor blockers. In in vitro studies with isolated organs and in binding studies on numerous receptors, E-4716 had no activity even at high concentrations, except for the selective blockade of H1 receptors. No activity was observed in pharmacological trials in vivo, such as the Irwin test or analgesia induced by phenylbenzoquinone or electroshock, suggesting a depressant activity on the CNS.

Author(s): 
Fisas, M. A.
Gutiérrez, B.
Fort, M.
Dordal, A.
García, C.
Farré, A. J.
Publication Title: 
Journal of Pharmacological Sciences

Nociceptin/orphanin FQ peptide (NOP)-receptor agonists have been shown to produce anxiolytic-like effects in rodents subjected to various behavioral assays. Recently, we developed a new nonpeptide agonist of the NOP receptor, 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole (MCOPPB), as an anxiolytic agent.

Author(s): 
Hirao, Akiko
Imai, Aki
Sugie, Yutaka
Yamada, Yoshinari
Hayashi, Shigeo
Toide, Katsuo
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

Human fascioliasis caused by Fasciola hepatica or Fasciola gigantica is an increasing global problem. The mainstay of current treatment is triclabendazole, but resistance in animals has been described, and it is not available in many countries. The antimalarial artesunate has an excellent safety profile, and there is increasing evidence of its efficacy against other parasites both in vitro and in vivo. We performed a study to investigate the usefulness of artesunate in symptomatic human fascioliasis; 100 patients were enrolled.

Author(s): 
Hien, Tran Tinh
Truong, Ng Thanh
Minh, Nguyen Hoang
Dat, Hoang Dinh
Dung, Nguyen Thi
Hue, Nguyen Thi
Dung, Tran Kim
Tuan, Phung Quoc
Campbell, James I.
Farrar, Jeremy J.
Day, Jeremy N.
Publication Title: 
Antimicrobial Agents and Chemotherapy

Triclabendazole resistance is continually documented from livestock, and hence new treatment strategies for Fasciola hepatica infections are needed. We investigated the effect of triclabendazole combined with artesunate, artemether, or OZ78 compared to that of monotherapy against adult and juvenile F. hepatica in rats. In vitro experiments with triclabendazole and its sulfoxide and sulfone metabolites, each in combination with the peroxides, complemented our study. F.

Author(s): 
Duthaler, Urs
Smith, Thomas A.
Keiser, Jennifer
Publication Title: 
Journal of Environmental Biology / Academy of Environmental Biology, India

A reliable and reproducible protocol for contamination free plant recovery system from alginated encapsulated uninodal microcuttings of micropropagated Bacopa monnieri L. have been developed after storage at 18 degrees C for 45 days. Node segments excised from freshly micropropagated plants were encapsulated as single explant beads with 3.0% sodium alginate and 80 mM CaCl2 2 H2O. To find out the optimal concentration of fungicide bavistin for efficient plant recovery different concentrations of bavistin (1.0 - 15 mg l(-1)) were incorporated in to the encapsulation medium.

Author(s): 
Ramseh, M.
Marx, R.
Mathan, G.
Pandian, S. Karutha
Publication Title: 
Atherosclerosis

INTRODUCTION: Toll-like receptors play an important role in the innate immune system and are found to be crucial in severe diseases like sepsis, atherosclerosis, and arthritis. TLR2 and TLR4 expression is upregulated in the inflammatory diseases. Angiotensin II in addition to stimulating vasoconstriction also induces an increase in ROS and a proinflammatory phenotype via AT(1)R. Angiotensin II type-1 receptor blocker (ARB), widely used as an antihypertensive drug, has been reported to also have anti-inflammatory effects.

Author(s): 
Dasu, Mohan R.
Riosvelasco, Andrea C.
Jialal, Ishwarlal
Publication Title: 
International Journal of Cardiology

BACKGROUND: ASCOT-BPLA study demonstrates that in hypertensive subjects, atenolol+bendroflumethiazide therapy is associated with higher incidence of adverse cardiovascular outcomes and developing diabetes than an amlodipine+perindopril regimen. This is not explained by changes in blood pressure alone. We hypothesized that distinct vascular and metabolic effects of anti-hypertensive drugs may explain these differential effects.

Author(s): 
Koh, Kwang Kon
Quon, Michael J.
Han, Seung Hwan
Lee, Yonghee
Kim, Soo Jin
Koh, Yesl
Shin, Eak Kyun
Publication Title: 
Translational Research: The Journal of Laboratory and Clinical Medicine

Mitochondrial membrane hyperpolarization and morphologic changes are important in inflammatory cell activation. Despite the pathophysiologic relevance, no valid and reproducible method for measuring mitochondrial homeostasis in human inflammatory cells is available currently. The purpose of this study was to define and validate reproducible methods for measuring relevant mitochondrial perturbations and to determine whether these methods could discern mitochondrial perturbations in type 2 diabetes mellitus (T2DM), which is a condition associated with altered mitochondrial homeostasis.

Author(s): 
Widlansky, Michael E.
Wang, Jingli
Shenouda, Sherene M.
Hagen, Tory M.
Smith, Anthony R.
Kizhakekuttu, Tinoy J.
Kluge, Matthew A.
Weihrauch, Dorothee
Gutterman, David D.
Vita, Joseph A.
Publication Title: 
PloS One

Prolonged hypoxic/ischemic stress may cause cortical injury and clinically manifest as a neurological disability. Activation of the δ-opioid receptor (DOR) may induce cortical protection against hypoxic/ischemic insults. However, the mechanisms underlying DOR protection are not clearly understood. We have recently found that DOR activation modulates the expression of microRNAs (miRNAs) in the kidney exposed to hypoxia, suggesting that DOR protection may involve a miRNA mechanism.

Author(s): 
Yang, Yilin
Zhi, Feng
He, Xiaozhou
Moore, Meredith L.
Kang, Xuezhi
Chao, Dongman
Wang, Rong
Kim, Dong H.
Xia, Ying
Publication Title: 
International Journal of Molecular Sciences

We investigated whether δ-opioid receptor (DOR)-induced neuroprotection involves the brain-derived neurotrophic factor (BDNF) pathway. We studied the effect of DOR activation on the expression of BDNF and other proteins in the cortex of C57BL/6 mice exposed to hypoxia (10% of oxygen) for 1-10 days.

Author(s): 
Tian, Xuesong
Hua, Fei
Sandhu, Harleen K.
Chao, Dongman
Balboni, Gianfranco
Salvadori, Severo
He, Xiaozhou
Xia, Ying

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