Ropivacaine Protects against Memory Impairment and Hippocampal Damage in a Rat Neurodegeneration Model
Conclusions: This study demonstrates that ropivacaine executes a protective action against KA-induced neuronal damage and apoptosis in vivo. Protective effects may be caused by glutamate level reduction, caspase-3 activation suppression, and MAPKs phosphorylation reduction. Our findings indicate that ropivacaine can ben efit prevention or treatment of glutamate excitotoxicity-related neurodegenerative diseases.Pharmacology 2018;102:307 –315 (Source: Pharmacology)
Source: Pharmacology - October 5, 2018 Category: Drugs & Pharmacology Source Type: research
MPT0B169 and MPT0B002, New Tubulin Inhibitors, Induce Growth Inhibition, G2/M Cell Cycle Arrest, and Apoptosis in Human Colorectal Cancer Cells
In this study, we investigated the effects of MPT0B169 and MPT0B002 on glioblastoma, breast, lung, and colorectal cancer (CRC) cell lines. A cell viability analysis showed that MPT0B169 and MPT0B002 were more effective in inhibiting the proliferation of COLO205 and HT29 CRC cells than U87MG and GBM8401 glioblastoma, MCF-7 and MDA-MB-231 breast cancer, and A549 lung cancer cells. MPT0B169 and MPT0B002 inhibited growth of COLO205 and HT29 cells in dose- and time-dependent manners. A colony-formation assay confirmed the growth inhibitory effects of MPT0B169 and MPT0B002 on COLO205 and HT29 cells. MPT0B169 and MPT0B002 disrupt...
Source: Pharmacology - September 18, 2018 Category: Drugs & Pharmacology Source Type: research
Melatonin Induces Osteoblastic Differentiation of Mesenchymal Stem Cells and Promotes Fracture Healing in a Rat Model of Femoral Fracture via Neuropeptide Y/Neuropeptide Y Receptor Y1 Signaling
In this study, mesenchymal stem cells (MSCs) were isolated from rat bone marrow and identified by flow cytometry. We found that MLT treatment upregulated the neuropeptide Y (NPY) and NPY receptor Y1 (NPY1R) expression, and promoted the proliferation and migration of MSCs, which was suppressed by BIBP3226, an inhibitor of NPY1R. Moreover, the levels of NPY and NPY1R in MSCs undergoing osteoblastic differentiation were upregulated after MLT administration. MLT-induced osteoblastic differentiation of MSCs was suppressed by BIBP3226 treatment, as evidenced by decreased levels of alkaline phosphatase (ALP), collagen type I α1 ...
Source: Pharmacology - September 18, 2018 Category: Drugs & Pharmacology Source Type: research
Sodium Houttuyfonate Inhibits Voltage-Gated Peak Sodium Current and Anemonia Sulcata Toxin II-Increased Late Sodium Current in Rabbit Ventricular Myocytes
Conclusions: The inhibitory effects of SH on ATX II-increased INa.L may underlie the electrophysiological mechanisms of the cardioprotective effects of SH; SH has the potential to be an effective and safe antiarrhythmic drug.Pharmacology 2018;102:253 –261 (Source: Pharmacology)
Source: Pharmacology - August 23, 2018 Category: Drugs & Pharmacology Source Type: research
A Novel, Nonpeptidic, Orally Active Bivalent Inhibitor of Human β-Tryptase
β-Tryptase is released from mast cells upon degranulation in response to allergic and inflammatory stimuli. Human tryptase is a homotetrameric serine protease with 4 identical active sites directed toward a central pore. These active sites present an optimized scenario for the rational design of bi valent inhibitors, which bridge 2 adjacent active sites. Using (3-[1-acylpiperidin-4-yl]phenyl)methanamine as the pharmacophoric core and a disiloxane linker to span 2 active sites we have successfully produced a novel bivalent tryptase inhibitor, compound 1a, with a comparable profile to previously described inhibitors. Pharma...
Source: Pharmacology - August 22, 2018 Category: Drugs & Pharmacology Source Type: research
