Collaborating with Alexander Scriabine and the Miles Institute for Preclinical Pharmacology

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• 作者：Ronald A. Janis ; ^{janisra@hotmail.com" class="auth_mail" title="E-mail the corresponding author} ; ^{Adottens@gmail.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Calcium channel drugs ; Potassium channel ligands ; Endogenous ligand ; Anandamide ; Endocannabinoid
• 刊名：Biochemical Pharmacology
• 出版年：2015
• 出版时间：15 November 2015
• 年：2015
• 卷：98
• 期：2
• 页码：318-321
• 全文大小：380 K

文摘

This article represents a timely opportunity to express my affection, admiration and gratitude to Professor David Triggle. David was my Ph.D. advisor as well as a key consultant in the 1980s and early 1990s for research programs at Miles Institute for Preclinical Pharmacology in West Haven, CT, the U.S. research operation of Bayer AG, in the areas of Ca²⁺ and K⁺ channel ligands. The binding methodology developed in his laboratory was used to search for an endogenous ligand for L-type Ca²⁺ channels. We did not find the substance that we were searching for, a genetically-determined, competitive inhibitor for the 1,4-dihydropyridine binding site, but instead isolated the endogenous ligand for the brain's own marijuana, anandamide. Devane, Mechoulam and coworkers first discovered that this compound was the endogenous ligand for delta-9-tetrahydrocannabinol, the active substance in cannabis. The endogenous endocannabinoid system is now the target of many exciting new approaches to drug discovery.