Everhardus Ariëns

Everhardus (Eef) Jacobus Ariëns (born January 29, 1918 in Wijk bij Duurstede ; † March 3, 2002 in Nijmegen ) was a Dutch pharmacologist and professor at the Katholieke Universiteit Nijmegen (now Radboud Universiteit Nijmegen). He made important contributions to the function of receptors and the mathematical description of ligand- receptor interactions ( receptor theory ). In addition, Everhardus Ariëns was the initiator for the introduction of stereochemistry into drug development and a pioneer in the development of enantiomerically pure drugs .

Life

youth

Everhardus Ariëns grew up as the sixth of ten children in Wijk bij Duurstede. After a temporary stay at boarding school, he obtained the general university entrance qualification in Wageningen in 1935 . He then took up a degree in chemistry at the University of Utrecht , which he graduated in 1942, although his preference was actually biology. Another study was interrupted by the Second World War. After refusing to sign a declaration of loyalty to the German Reich and fleeing the German-occupied Netherlands via Switzerland, France and England, Everhardus Ariëns joined the US Army . He completed his medical studies after the Second World War in 1948.

Scientific activity

After the Second World War, he carried out research in the group of Prof. UG Bijlsma in the field of adrenergic substances and received his doctorate in both chemistry and medicine in 1950 . In 1951 Everhardus Ariëns moved to Nijmegen after a faculty for pharmacology had been established at the Catholic University there. From 1954 until his retirement he was a professor there.

Based on his dissertations , he and Jacques van Rossum developed a method to quantify pharmacological effects as a result of ligand-receptor interactions. To this end, he introduced the terms affinity and intrinsic activity . With the help of these terms he was able to describe the behavior of agonists and antagonists as well as the dual agonist / antagonist behavior of partial agonists . An important merit of Ariëns was the establishment of experiments on isolated organs instead of living animals, which quickly and reproducibly provided information about the affinity and intrinsic activity of test substances.

Everhardus Ariëns was also active in the field of structure-activity relationships (SAR), a branch of medicinal chemistry . With the provocative statement that the racemates commonly used at that time were drugs with 50% contamination, he triggered a discussion among pharmacologists and medical chemists and alerted the drug approval authorities. Everhardus Ariëns was thus the decisive pioneer for the targeted development of enantiomerically pure medicinal substances. He started another controversy, albeit less publicized, by expressing his view that drug metabolism was wasteful and called for the development of metabolism-resistant drugs. In addition, in the tradition of Dutch pharmacologists, he campaigned for the fight against quackery .

honors and awards

Everhardus Ariëns was awarded the Purkinje Medal at the second International Pharmacology Congress in Prague in 1963. He also received the Dr. Saal van Zwanenberg Prize (1972), the Poulsson Medal of the Norwegian Pharmacological Society (1973), the Scheele Medal (1974), the Schmiedeberg Plaque (1980) and the Smissman Award the American Chemical Society (1985).

In 1974 he was elected a member of the Leopoldina . Everhardus Ariëns was from the universities Universidade Luterana do Brasil , University of Kiel , University of Paris-South and Università degli Studi di Camerino the honorary doctorate awarded. Another honorary doctorate was scheduled for March 22, 2002 at Ohio State University .

Fonts

• Molecular Pharmacology . Elsevier Science & Technology Books, San Diego, CA, 1967, ISBN 0120604019

Individual evidence

1. ^ ^{A b} H. Timmerman, DD Breimer: Everhardus Jacobus Ariëns . Koninglijke Nederlandse Akademie van Wetenschappen. www.knaw.nl/publicaties/pdf/20061074_1.pdf
2. ↑ ^{a b} P. N. Patil: Everhardus J. Ariens (1918-2002). A tribute . In: Trends in Pharmacological Sciences . Volume 23, 2002, pp. 344-345.
3. ^ EJ Ariens, JM van Rossum, AM Simonis: Affinity, intrinsic activity and drug interactions . In: Pharmacol. Rev. . 9, No. 2, June 1957, pp. 218-236. PMID 13465302 .
4. ^ EJ Ariëns: Stereochemistry, a basis for sophisticated nonsense in pharmacokinetics and clinical pharmacology . In: Eur. J. Clin. Pharmacol. . 26, No. 6, 1984, pp. 663-668. PMID 6092093 .
5. ↑ Member entry of Everardus Jacobus Ariëns at the German Academy of Natural Scientists Leopoldina , accessed on December 28, 2015.