7 research outputs found
Dissociation Rates as One of the Differentiating Factors for Hyperthermic and Non-Hyperthermic TRPV1 Antagonists
Preventive effects of naldemedine, peripherally acting μ-opioid receptor antagonist, on morphine-induced nausea and vomiting in ferrets
Automatic Operation System of Cable Crane for Concrete Dams : 1st Report, Large-Scale Experimental Model and Simulation Model of Cable Crane
Automatic Operation System of Cable Crane for Concrete Dams : 2nd Report, Anti-Sway Control and Anti-Rebound Control
Automatic Operation System of Cable Crane for Concrete Dams : 2nd Report, Anti-Sway Control and Anti-Rebound Control
O presente artigo é produto de uma pesquisa empreendida sobre as revoltas de escravos ocorridas em fins da República Romana e seu significado. Ela resume a dissertaçao de mestrado redigida recentemente sobre o tema e foi apresentado como comunicaçao no XXI Ciclo de Debates do LHIA/UFRJ. Este artigo tenta dar conta de seus aspectos centrais, bem como divulgar o estudo realizado para provocar o debate
Structure–Activity Relationship Studies and Discovery of a Potent Transient Receptor Potential Vanilloid (TRPV1) Antagonist 4‑[3-Chloro-5-[(1<i>S</i>)‑1,2-dihydroxyethyl]-2-pyridyl]‑<i>N</i>‑[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro‑2<i>H</i>‑pyridine-1-carboxamide (V116517) as a Clinical Candidate for Pain Management
A series of novel tetrahydropyridinecarboxamide
TRPV1 antagonists
were prepared and evaluated in an effort to optimize properties of
previously described lead compounds from piperazinecarboxamide series.
The compounds were evaluated for their ability to block capsaicin
and acid-induced calcium influx in CHO cells expressing human TRPV1.
The most potent of these TRPV1 antagonists were further characterized
in pharmacokinetic, efficacy, and body temperature studies. On the
basis of its pharmacokinetic, in vivo efficacy, safety, and toxicological
properties, compound <b>37</b> was selected for further evaluation
in human clinical trials