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Design and synthesis of the first indole-based blockers of Panx-1 channel
We present here a study aimed at obtaining the first class of selective Panx-1 blockers, a new topic for pharmaceutical chemistry, since all compounds used so far for the study of this channel have different primary targets. Among various scaffolds analyzed, the indole nucleous emerged, whose elaboration yielded interesting Panx-1 blockers, such as the potent 5-sulfamoyl derivatives 14c and 15b (I% = 100 at 50 μM). In vivo tests performed in the mouse model of oxaliplatin-induced neuropathy, demonstrated that the hypersensitivity was completely reverted by treatment with 15b (1 nmol, administered intrathecally), suggestin...
Source: European Journal of Medicinal Chemistry - June 26, 2021 Category: Chemistry Authors: Letizia Crocetti Gabriella Guerrini Sara Puglioli Maria Paola Giovannoni Lorenzo Di Cesare Mannelli Elena Lucarini Carla Ghelardini Junjie Wang Gerhard Dahl Source Type: research

Chemotherapy induced stroke mimic: 5-Fluorouracil encephalopathy fulfilling criteria for tissue plasminogen activator therapy
Stroke mimics, especially those involving chemotherapy related neurotoxicity, can confound the clinical diagnosis of acute stroke. Here we describe the case of a 63year-old male with a recent history of stage IIIC colon cancer who presented with confusion on the second day of modified FOLFOX6 (5-fluorouracil/oxaliplatin) chemotherapy and subsequently received alteplase, tissue plasminogen activator therapy (tPA), for presumed ischemic stroke. Magnetic resonance imaging scans after tPA administration did not reveal evidence of an infarction and the patients' neurological symptoms resolved completely after discontinuation of...
Source: The American Journal of Emergency Medicine - July 6, 2017 Category: Emergency Medicine Authors: May Thuy Nguyen, Robyn Stoianovici, Luigi Brunetti Source Type: research