ESPD 50

Ethnopharmacologic Search for Psychoactive Drugs

ESPD 50
SPEAKERS

David E. Nichols

David E. Nichols

Ethnopharmacologist

“From “There” to “Here””

read the transcript

“an excursion that considers each of the major types of psychedelic agents: tryptamines, ergolines, and phenethylamines”

Biography

Prior to his retirement in June 2012, he was the Robert C. and Charlotte P. Anderson Distinguished Chair in Pharmacology at the Purdue University College of Pharmacy, and also was adjunct Professor of Pharmacology at the Indiana University School of Medicine. He is currently an Adjunct Professor at the University of North Carolina Chapel Hill, NC, where he continues his research. In 2004 he was named the Irwin H. Page Lecturer, and in 2006 was named the first Provost’s s Outstanding Graduate Mentor at Purdue. The focus of his graduate training, beginning in 1969, and of much of his research subsequent to receiving his doctorate in 1973 has been the investigation of the relationship between molecular structure and the action of psychedelic agents and other substances that modify behavioral states. Widely published in the scientific literature and internationally recognized for his research on centrally active drugs, he has studied all of the major classes of psychedelic agents.Among scientists, he is recognized as one of the foremost experts on the medicinal chemistry of hallucinogens.

“From “There” to “Here””

… natural product templates (“there”), and how each template evolved through chemical structural modification that led either to optimized potency or unique psychopharmacology (“here”)

Transcript abstract

This talk will be an excursion that considers each of the major types of psychedelic agents: tryptamines, ergolines, and phenethylamines. The talk will feature natural product templates (“there”), and show how each template evolved through chemical structural modification that led either to optimized potency or unique psychopharmacology (“here”). Each chemotype has at some point in time been the focus of attention by natural products or medicinal chemists. For example, in the “modern” era, Western attention to psychedelics was first directed to mescaline, a simple trimethoxy-substituted phenethylamine produced by the peyote cactus, Lophophora wiliamsii. Anthropological studies have indicated the use of peyote by Native North Americans was ongoing as long as 5700 years ago. Following the identification of mescaline as the active component in peyote by Heffter in 1897, it was then synthesized in 1919 by Späth. More than four decades would then pass before the prodigious efforts of Alexander Shulgin led to a variety of ring-substituted analogues of mescaline. Part of Shulgin’s inspiration derived from his knowledge of the structures of essential oils. Additional medicinal chemistry efforts led to extremely potent congeners of mescaline. Similar, although less productive, studies occurred with simple tryptamines and with the tetracyclic ergolines. Each of these chemotypes will be discussed and it will be seen how natural products played a significant role in bringing psychedelics of various types to the present moment (“here”).