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Pharmacology of Novel Fentanyls Revealed

Thursday, June 25, 2020   (0 Comments)
Posted by: Alisha Brown
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The binding affinity and efficacy of 34 fentanyl analogs were determined through a collaboration between Cayman Chemical’s Division of Forensic Science and the Edward F. Domino Research Center in the Department of Pharmacology of the University of Michigan. “Pharmacological data was lacking for the host of fentanyl analogs that have erupted onto the illicit market during the current opioid epidemic,” said Sherif Hassanien, liaison of the collaboration between Cayman and U-M. “A cohesive understanding of each fentanyl analog’s in vitro pharmacology is absolutely necessary for the development of policies and notices issued by law enforcement and public health agencies. It’s also important for research conducted by academic institutes.”

Cayman produced and supplied the laboratory of U-M’s Dr. John Traynor with analytical opioid standards, which were studied using in vitro receptor binding assays and functional assays (including the human μ-opioid receptor). The list of compounds comprised scheduled fentanyls—both classically known and novel to the illicit market. The results have been published in Drug Testing and Analysis. “Our work, which was supported by grants from the National Institute on Drug Abuse, shows a wide range of potencies and efficacies across the compounds that will aid in understanding structure-activity relationships of the fentanyl scaffold," said Jessica Anand, PhD, Research Investigator in Pharmacology at U-M and lead scientist on the study, "moreover, the information will help federal agencies make scheduling decisions."

This study offers one of the first comprehensive publications on the human in vitro pharmacology of fentanyls and could provide preliminary insights on their activity in the human body. “There are an infinite amount of fentanyl analogs that can be made and distributed, but this sample set at least gives some insight to the scientific community about their potential dangers to human health,” said Jon Bassman, a Cayman chemist who also worked on the project. With the rapid rise in deaths due to fentanyl abuse, this information will provide needed insight to protection precautions for field and lab safety, lead to the discovery of safer analgesics, and serve the development of research tools to probe signaling pathways.

About Cayman Chemical
Cayman Chemical Company helps make research possible by supplying scientists worldwide with biochemical tools used to understand cancerneurochemistryoxidative injuryendocrinologyatherosclerosis, and other human health challenges. We are a leader in the field of designer drugs by providing high-purity reference standards to federally licensed laboratories and qualified academic research institutions for forensic analysis. Our highly trained staff of chemists provides institutions with solutions to quickly identify and understand the physiological and toxicological properties of new designer drugs. Cayman synthesizes a range of analytical standards including synthetic cannabinoids, cathinones, phenethylamines, amphetamines, indanes, opioids, benzodiazepines, tryptamines, and phytocannabinoids, among many others. In addition, Cayman Contract Services provides discovery and pre-clinical development services to the global pharmaceutical, biotechnology, and academic research markets. Our diverse suite of services leverages a team of over 150 highly skilled scientists with expertise in medicinal chemistry, structure-based drug design, complex multi-step organic synthesis, analytical chemistry, sample analysis, and custom assay development. Cayman performs generic drug development and production in both Ann Arbor, Michigan and Neratovice, Czech Republic.

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