Everhardus Jacobus Ariëns
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Everhardus Jacobus Ariëns (29 January 1918 – 3 March 2002) was a Dutch
pharmacologist Pharmacology is a branch of medicine, biology and pharmaceutical sciences concerned with drug or medication action, where a drug may be defined as any artificial, natural, or endogenous (from within the body) molecule which exerts a biochemic ...
and professor at the Catholic University of Nijmegen (now Radboud University Nijmegen). He made important contributions to the function of
receptors Receptor may refer to: *Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a n ...
and the mathematical description 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 of a receptor that ...
). Moreover, Everhardus Ariëns was the initiator for the collection of stereochemistry 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 re ...
and spearheading the development of
enantiopure In chemistry, an enantiomer ( /ɪˈnænti.əmər, ɛ-, -oʊ-/ ''ih-NAN-tee-ə-mər''; from Ancient Greek ἐνάντιος ''(enántios)'' 'opposite', and μέρος ''(méros)'' 'part') – also called optical isomer, antipode, or optical anti ...
drugs.


Early life

Everhardus Ariëns grew up as the sixth of ten children in
Wijk bij Duurstede Wijk bij Duurstede () is a 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 Duurstede, 2013.'' City The city ...
. After a temporary boarding school experience, in 1935 he was admitted to Wageningen, the general university. Then he took a degree in chemistry at the
University of Utrecht Utrecht University (UU; nl, Universiteit Utrecht, formerly ''Rijksuniversiteit Utrecht'') is a public research university in Utrecht, Netherlands. Established , it is one of the oldest universities in the Netherlands. In 2018, it had an enrollme ...
in which he completed in 1942, although his preference was actually the biology. Another study was interrupted by the Second World War. After his refusal to sign a declaration of loyalty to the German Reich and an escape from the Germany occupied Netherlands via Switzerland, France and England, he found asylum with the U.S. Army. He completed the unfinished part of his studies medicine 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, Everhardus 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 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 to its mol ...
. 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 ''Ex vivo'' (Latin: "out of the living") literally means that which takes place outside an organism. In science, ''ex vivo'' refers to experimentation or measurements done in or on tissue from an organism in an external environment with minimal ...
''), which quickly and reproducibly delivered data on 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 Medicinal or pharmaceutical chemistry is a scientific discipline at the intersection of chemistry and pharmacy involved with designing and developing pharmaceutical drugs. Medicinal chemistry involves the identification, synthesis and developme ...
. With the provocative statement that the then commonly used
racemate In chemistry, a racemic mixture, or racemate (), is one that has equal amounts 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 racemates. ...
s were drugs with 50% contamination. he triggered a debate among pharmacologists and medicinal chemists and alerted the drug regulators. Everhardus 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

Everhardus 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. 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). Everhardus Ariëns was awarded honorary doctorates from universities
Universidade Luterana do Brasil The Lutheran University of Brazil (Portuguese: or ULBRA) is a university which covers several states throughout Brazil. History The university has its roots in the parish school of St. Paul's Lutheran Church of Canoas (CELSP), in Canoas, Rio ...
,
University of Kiel Kiel University, officially the Christian-Albrecht University of Kiel, (german: Christian-Albrechts-Universität zu Kiel, abbreviated CAU, known informally as Christiana Albertina) is a university in the city of Kiel, Germany. It was founded in ...
,
University of Paris-Sud Paris-Sud University (French: ''Université Paris-Sud''), also known as University of Paris — XI (or as Université d'Orsay before 1971), was a French research university distributed among several campuses in the southern suburbs of Paris, in ...
and Università degli Studi di Camerino. Another honorary doctorate was awarded in March 2002 at the
Ohio State University The Ohio State University, commonly called Ohio State or OSU, is a public land-grant research university in Columbus, Ohio. A member of the University System of Ohio, it has been ranked by major institutional rankings among the best publ ...
.


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