Everhardus Jacobus Ariëns
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Everhardus Jacobus Ariëns (29 January 1918 – 3 March 2002) was a Dutch
pharmacologist Pharmacology is the science of drugs and medications, including a substance's origin, composition, pharmacokinetics, pharmacodynamics, therapeutic use, and toxicology. More specifically, it is the study of the interactions that occur between ...
and professor at the Catholic University of Nijmegen (now Radboud University Nijmegen). He made significant contributions to understanding
receptors Receptor may refer to: *Sensory receptor, in physiology, any neurite structure that, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds ...
function and the mathematical modeling of ligand–receptor interactions (
receptor theory Receptor theory is the application of receptor models to explain drug behavior. Pharmacological receptor models preceded accurate knowledge of receptors by many years. John Newport Langley and Paul Ehrlich introduced the concept that receptors ca ...
). Additionally, Ariëns was a pioneer in considering
stereochemistry Stereochemistry, a subdiscipline of chemistry, studies the spatial arrangement of atoms that form the structure of molecules and their manipulation. The study of stereochemistry focuses on the relationships between stereoisomers, which are defined ...
in
drug development Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. It includes preclinical research on microorganisms and animals, filing for regu ...
, including the development of
enantiopure In chemistry, an enantiomer ( /ɪˈnænti.əmər, ɛ-, -oʊ-/ ''ih-NAN-tee-ə-mər''), also known as an optical isomer, antipode, or optical antipode, is one of a pair of molecular entities which are mirror images of each other and non-superpos ...
drugs.


Early life

Ariëns grew up as the sixth of ten children in
Wijk bij Duurstede Wijk bij Duurstede () is a Municipalities of the Netherlands, municipality and a city in the central Netherlands. Population centres *Cothen *Langbroek *Wijk bij Duurstede Topography ''Dutch Topographic map of the municipality of Wijk bij Du ...
. He went to school in Wageningen. Then he studied medicine at the
University of Utrecht Utrecht University (UU; , formerly ''Rijksuniversiteit Utrecht'') is a public research university in Utrecht, Netherlands. Established , it is one of the oldest universities in the Netherlands. In 2023, it had an enrollment of 39,769 students, a ...
, followed by a doctorate of chemistry which he completed in 1942. After refusing to sign a declaration of loyalty to Germany, he escaped from the occupied Netherlands via Switzerland to England, where he enlisted in the U.S. Army. He completed his medical studies after the Second World War.


Scientific activity

After World War II he worked in the laboratory of Prof. UG Bijlsma in the area of
adrenergic Adrenergic means "working on adrenaline (epinephrine) or noradrenaline (norepinephrine)" (or on their receptors). When not further qualified, it is usually used in the sense of enhancing or mimicking the effects of epinephrine and norepinephrine ...
substances and in 1950 both in the field of chemistry and medical doctorate. In 1951, Ariëns moved to Nijmegen after there at the Catholic University of the Faculty of Pharmacology was established. From 1954 until his retirement he was employed there as a professor. Based on his dissertation, he developed together with Jacques van Rossum, a method for quantification of pharmacological effects as a result of ligand-receptor interactions. The thesis developed the concepts of receptor affinity and
intrinsic activity Intrinsic activity (IA) and efficacy (Emax) refer to the relative ability of a drug- receptor complex to produce a maximum functional response. This must be distinguished from the affinity, which is a measure of the ability of the drug to bind ...
. With the help of these terms he could describe the behavior of agonists and antagonists as well as the dual agonist / antagonist behavior of partial agonists. An important accomplishment of Ariëns was the establishment of experiments on isolated organs instead of the living animal (''
ex vivo refers to biological studies involving tissues, organs, or cells maintained outside their native organism under controlled laboratory conditions. By carefully managing factors such as temperature, oxygenation, nutrient delivery, and perfusi ...
''), which quickly and reproducibly delivered data on the affinity and intrinsic activity of test substances. Ariëns was also active in the field of structure-activity relationships (SAR), a branch of
medicinal chemistry Medicinal or pharmaceutical chemistry is a scientific discipline at the intersection of chemistry and pharmacy involved with drug design, designing and developing pharmaceutical medication, drugs. Medicinal chemistry involves the identification, ...
. With the provocative statement that the then commonly used
racemate In chemistry, a racemic mixture or racemate () is a mixture that has equal amounts (50:50) of left- and right-handed enantiomers of a chiral molecule or salt. Racemic mixtures are rare in nature, but many compounds are produced industrially as r ...
s were drugs with 50% contamination, he triggered a debate among pharmacologists and medicinal chemists and alerted drug regulators. Ariëns was thus the crucial precursor for the targeted development of enantiopure drugs. Another, though less noticed controversy he started by expressing his view that drug metabolism is wasted and called for the development of metabolism-resistant drugs. In addition, he followed in the tradition of Dutch pharmacists to combat quackery.


Honors and awards

Ariëns 1963 was honored at the second International Congress of Pharmacology in Prague with the Purkinje Medal. In 1970 he became member of the
Royal Netherlands Academy of Arts and Sciences The Royal Netherlands Academy of Arts and Sciences (, KNAW) is an organization dedicated to the advancement of science and literature in the Netherlands. The academy is housed in the Trippenhuis in Amsterdam. In addition to various advisory a ...
. He also received the Dr. Saal van Zwanenberg Award (1972), the Medal of the Norwegian Poulsson Pharmacological Society (1973), the Scheele Award (1974), the Schmiedeberg Medal (1980) and the Smissman Award of the American Chemical Society (1985). Ariëns was awarded honorary doctorates from universities Universidade Luterana do Brasil,
University of Kiel Kiel University, officially the Christian Albrecht University of Kiel, (, abbreviated CAU, known informally as Christiana Albertina) is a public research university in the city of Kiel, Germany. It was founded in 1665 as the ''Academia Holsator ...
,
University of Paris-Sud Paris-Sud University (), also known as the University of Paris — XI (or as the Orsay Faculty of Sciences, University of Paris before 1971), was a French research university distributed among several campuses in the southern suburbs of Paris, ...
and Università degli Studi di Camerino. Another honorary doctorate was awarded in March 2002 at the
Ohio State University The Ohio State University (Ohio State or OSU) is a public university, public Land-grant university, land-grant research university in Columbus, Ohio, United States. A member of the University System of Ohio, it was founded in 1870. It is one ...
.


References


Further reading

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External links

* {{DEFAULTSORT:Ariens, Everhardus Jacobus 1918 births 2002 deaths Dutch pharmacologists Members of the Royal Netherlands Academy of Arts and Sciences People from Wijk bij Duurstede Utrecht University alumni Academic staff of Radboud University Nijmegen Stereochemists