Published June 3, 2015
Two expert reviewers for the global literature review service F1000Prime have recommended a University at Buffalo paper identifying molecular mechanisms affected by the local anesthetic bupivacaine.
The paper, “Actions of Bupivacaine, a Widely Used Local Anesthetic, on NMDA Receptor Responses,” was published in the Journal of Neuroscience.
Paganelli was a National Institutes of Health predoctoral fellow.
The article received two out of three stars — or a “very good” rating — from two evaluators with the post-publication peer review service.
Their recommendations cite the research for its new finding and interesting hypothesis.
“The research may have implications for treating chronic pain and perhaps acute pain, as well as preventing the transition from acute to chronic pain,” says Darin Correll, MD. He is an expert on anesthesiology and pain management and assistant professor at Harvard Medical School.
The study is the first to investigate how bupivacaine inhibits the action of N-methyl-D-aspartate (NMDA) glutamate receptor proteins in the spinal cord.
This synaptic protein gates an ionic current across the cellular membrane upon binding the neurotransmitter glutamate. It plays a pivotal role in the neurological disease state of chronic pain.
“These authors show that bupivacaine ... inhibits NMDA receptors by a sequential or ‘foot-in-the-door’ blocking mechanism, in which the drug prevents ion channel closing, and that it also affects gating by an allosteric [non-chemically active binding-site] mechanism,” notes Robert W. Peoples, PhD.
“Interestingly, bupivacaine acts via both extracellular and intracellular sites, and can associate with or dissociate from these sites whether the channel is open or closed,” Peoples adds.
He is an expert in pharmacology and drug discovery and associate professor of biomedical sciences at Marquette University in Milwaukee.
Through F1000Prime, more than 5,800 top scientists and their associates select and evaluate the published papers they find most interesting and noteworthy in their fields.
Altogether, they review an average of 1,500 papers each month, culled from more than 3,500 journals — approximately the top 2 percent of all articles published in medicine and the life sciences.
Their reviews are posted online for F1000Prime subscribers.