BernheimV1, Main, Exploration, bibRecord, 000C81

Deprenyl (selegiline): the history of its development and pharmacological action

Identifieur interne : 000C81 ( Main/Exploration ); précédent : 000C80; suivant : 000C82

Deprenyl (selegiline): the history of its development and pharmacological action

Auteurs : J. Knoll [Hongrie]

Source :

Acta Neurologica Scandinavica [ 0001-6314 ] ; 1983-07.

RBID : ISTEX:960D57F059B0F695D1B886989BE8CA37D6F1BFB5

English descriptors

Teeft :
- Acta, Ageing, Ageing brain, Amine, Amphetamine, Antidepressant, Basal ganglia, Biochem, Bipolar, Birkmayer, Cheese effect, Clinical practice, Clorgyline, Continuous administration, Daily administration, Deprenyl, Deprenyl treatment, Dopamine, Dopaminergic, Dopaminergic activity, Dopaminergic modulation, Dopaminergic neurons, Dopaminergic system, Dopaminergic tone, Dos, Endogenous, Fractional rate, Human brain, Hypertensive, Inhibitor, Isomer, Knoll, Lancet, Levodopa, Levodopa treatment, Madopar, Magyar, Male rats, Methamphetamine, Modern problems, Monoamine, Monoamine oxidase, Monoamine oxidase inhibitors, Monoamine oxidases, Nerve terminals, Neural transm, Neuron, Noradrenaline, Other hand, Oxidase, Pargyline, Parkinsonian, Parkinsonian patients, Parkinsonian symptoms, Peripheral decarboxylase inhibitor, Pharmacol, Pharmacological, Pharmacological activity, Pharmacological influences, Pharmacology, Postsynaptic, Present time, Racemic, Raven press, Receptor, Riederer, Sandler, Selective inhibition, Selective inhibitor, Selective inhibitors, Selegiline, Serotonergic, Sexual activity, Sexual events, Sexual performance, Sexual vigour, Striatum, Transm, Tranylcypromine, Turnover, Turnover rate, Tyramine, Vigour, Vizi, Youdim.

Abstract

ABSTRACT — Deprenyl inhibits MAO‐B selectively in different animal species and in man. Its safety margin is remarkable. We were able to block MAO‐B activity in the brain selectively in vivo in four species (mouse, rat, cat, dog) with s.c. administration of 0.17–0.31% of LD50. The usual oral dose range in clinical practice, 5–20 mg daily (0.05–0.2 mg/kg), is about ten times lower than the orally active dose in the rat.

Deprenyl proved to be a safe drug in man. Neither hypertensive reactions nor the need for any special dietary care were ever encountered during long‐term (2–8 years) daily administration of the drug.

The most important effect of deprenyl in the brain is the sensitization of dopaminergic neurons to physiological and pharmacological influences, but in contrast to levodopa or bromocrytine, deprenyl does not elicit an acute increase in dopaminergic activity. The effect of deprenyl is due, on the one hand, to the inhibition of MAO‐B and, on the other hand, to inhibition of the uptake of dopamine.

In agreement with its peculiar spectrum of pharmacological activity, deprenyl proved to be a useful adjuvant to levodopa alone or in combination with a peripheral decarboxylase inhibitor. In addition, a supplement of deprenyl in Parkinson's disease led to significant prolongation of the duration of the illness. This has not been observed so far with other antiparkinsonian drugs.

The dopamine content of the human caudate nucleus decreases by 13 % per decade over the age of 45.

The hypothesis has been put forward that the significant increase of incidence of depression in the elderly, the age‐dependent decline in male sexual vigour and the frequent appearance of parkinsonian symptoms in the later decades of life might be attributed to a decrease of dopamine and ‘trace amines’ in the brain. The possibility of countering these biochemical lesions of ageing by long‐term administration of deprenyl, a selective inhibitor of MAO‐B which facilitates dopaminergic and ‘trace‐aminergic’ activity in the brain, and is a safe drug in man, is considered in detail.

Url:

https://api.istex.fr/document/960D57F059B0F695D1B886989BE8CA37D6F1BFB5/fulltext/pdf

DOI: 10.1111/j.1600-0404.1983.tb01517.x

Affiliations:

Links toward previous steps (curation, corpus...)

to stream Istex, to step Corpus: 000E26
to stream Istex, to step Curation: 000E25
to stream Istex, to step Checkpoint: 000952
to stream Main, to step Merge: 000C95
to stream Main, to step Curation: 000C81

Le document en format XML

<record><TEI wicri:istexFullTextTei="biblStruct"><teiHeader><fileDesc><titleStmt><title xml:lang="en">Deprenyl (selegiline): the history of its development and pharmacological action</title>
<author><name sortKey="Knoll, J" sort="Knoll, J" uniqKey="Knoll J" first="J." last="Knoll">J. Knoll</name>
</author>
</titleStmt>
<publicationStmt><idno type="wicri:source">ISTEX</idno>
<idno type="RBID">ISTEX:960D57F059B0F695D1B886989BE8CA37D6F1BFB5</idno>
<date when="1983" year="1983">1983</date>
<idno type="doi">10.1111/j.1600-0404.1983.tb01517.x</idno>
<idno type="url">https://api.istex.fr/document/960D57F059B0F695D1B886989BE8CA37D6F1BFB5/fulltext/pdf</idno>
<idno type="wicri:Area/Istex/Corpus">000E26</idno>
<idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Corpus" wicri:corpus="ISTEX">000E26</idno>
<idno type="wicri:Area/Istex/Curation">000E25</idno>
<idno type="wicri:Area/Istex/Checkpoint">000952</idno>
<idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Checkpoint">000952</idno>
<idno type="wicri:doubleKey">0001-6314:1983:Knoll J:deprenyl:selegiline:the</idno>
<idno type="wicri:Area/Main/Merge">000C95</idno>
<idno type="wicri:Area/Main/Curation">000C81</idno>
<idno type="wicri:Area/Main/Exploration">000C81</idno>
</publicationStmt>
<sourceDesc><biblStruct><analytic><title level="a" type="main">Deprenyl (selegiline): the history of its development and pharmacological action</title>
<author><name sortKey="Knoll, J" sort="Knoll, J" uniqKey="Knoll J" first="J." last="Knoll">J. Knoll</name>
<affiliation wicri:level="3"><country xml:lang="fr">Hongrie</country>
<wicri:regionArea>Department of Pharmacology, Semmelweis University of Medicine, Budapest</wicri:regionArea>
<placeName><settlement type="city">Budapest</settlement>
<region nuts="2">Hongrie centrale</region>
</placeName>
</affiliation>
<affiliation wicri:level="1"><country xml:lang="fr">Hongrie</country>
<wicri:regionArea>Correspondence address: Address: </wicri:regionArea>
</affiliation>
</author>
</analytic>
<monogr></monogr>
<series><title level="j" type="main">Acta Neurologica Scandinavica</title>
<title level="j" type="alt">ACTA NEUROLOGICA SCANDINAVICA</title>
<idno type="ISSN">0001-6314</idno>
<idno type="eISSN">1600-0404</idno>
<imprint><biblScope unit="vol">68</biblScope>
<biblScope unit="page" from="57">57</biblScope>
<biblScope unit="page" to="80">80</biblScope>
<biblScope unit="page-count">24</biblScope>
<publisher>Blackwell Publishing Ltd</publisher>
<pubPlace>Oxford, UK</pubPlace>
<date type="published" when="1983-07">1983-07</date>
</imprint>
<idno type="ISSN">0001-6314</idno>
</series>
</biblStruct>
</sourceDesc>
<seriesStmt><idno type="ISSN">0001-6314</idno>
</seriesStmt>
</fileDesc>
<profileDesc><textClass><keywords scheme="Teeft" xml:lang="en"><term>Acta</term>
<term>Ageing</term>
<term>Ageing brain</term>
<term>Amine</term>
<term>Amphetamine</term>
<term>Antidepressant</term>
<term>Basal ganglia</term>
<term>Biochem</term>
<term>Bipolar</term>
<term>Birkmayer</term>
<term>Cheese effect</term>
<term>Clinical practice</term>
<term>Clorgyline</term>
<term>Continuous administration</term>
<term>Daily administration</term>
<term>Deprenyl</term>
<term>Deprenyl treatment</term>
<term>Dopamine</term>
<term>Dopaminergic</term>
<term>Dopaminergic activity</term>
<term>Dopaminergic modulation</term>
<term>Dopaminergic neurons</term>
<term>Dopaminergic system</term>
<term>Dopaminergic tone</term>
<term>Dos</term>
<term>Endogenous</term>
<term>Fractional rate</term>
<term>Human brain</term>
<term>Hypertensive</term>
<term>Inhibitor</term>
<term>Isomer</term>
<term>Knoll</term>
<term>Lancet</term>
<term>Levodopa</term>
<term>Levodopa treatment</term>
<term>Madopar</term>
<term>Magyar</term>
<term>Male rats</term>
<term>Methamphetamine</term>
<term>Modern problems</term>
<term>Monoamine</term>
<term>Monoamine oxidase</term>
<term>Monoamine oxidase inhibitors</term>
<term>Monoamine oxidases</term>
<term>Nerve terminals</term>
<term>Neural transm</term>
<term>Neuron</term>
<term>Noradrenaline</term>
<term>Other hand</term>
<term>Oxidase</term>
<term>Pargyline</term>
<term>Parkinsonian</term>
<term>Parkinsonian patients</term>
<term>Parkinsonian symptoms</term>
<term>Peripheral decarboxylase inhibitor</term>
<term>Pharmacol</term>
<term>Pharmacological</term>
<term>Pharmacological activity</term>
<term>Pharmacological influences</term>
<term>Pharmacology</term>
<term>Postsynaptic</term>
<term>Present time</term>
<term>Racemic</term>
<term>Raven press</term>
<term>Receptor</term>
<term>Riederer</term>
<term>Sandler</term>
<term>Selective inhibition</term>
<term>Selective inhibitor</term>
<term>Selective inhibitors</term>
<term>Selegiline</term>
<term>Serotonergic</term>
<term>Sexual activity</term>
<term>Sexual events</term>
<term>Sexual performance</term>
<term>Sexual vigour</term>
<term>Striatum</term>
<term>Transm</term>
<term>Tranylcypromine</term>
<term>Turnover</term>
<term>Turnover rate</term>
<term>Tyramine</term>
<term>Vigour</term>
<term>Vizi</term>
<term>Youdim</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract">ABSTRACT — Deprenyl inhibits MAO‐B selectively in different animal species and in man. Its safety margin is remarkable. We were able to block MAO‐B activity in the brain selectively in vivo in four species (mouse, rat, cat, dog) with s.c. administration of 0.17–0.31% of LD50. The usual oral dose range in clinical practice, 5–20 mg daily (0.05–0.2 mg/kg), is about ten times lower than the orally active dose in the rat.</div>
<div type="abstract">Deprenyl proved to be a safe drug in man. Neither hypertensive reactions nor the need for any special dietary care were ever encountered during long‐term (2–8 years) daily administration of the drug.</div>
<div type="abstract">The most important effect of deprenyl in the brain is the sensitization of dopaminergic neurons to physiological and pharmacological influences, but in contrast to levodopa or bromocrytine, deprenyl does not elicit an acute increase in dopaminergic activity. The effect of deprenyl is due, on the one hand, to the inhibition of MAO‐B and, on the other hand, to inhibition of the uptake of dopamine.</div>
<div type="abstract">In agreement with its peculiar spectrum of pharmacological activity, deprenyl proved to be a useful adjuvant to levodopa alone or in combination with a peripheral decarboxylase inhibitor. In addition, a supplement of deprenyl in Parkinson's disease led to significant prolongation of the duration of the illness. This has not been observed so far with other antiparkinsonian drugs.</div>
<div type="abstract">The dopamine content of the human caudate nucleus decreases by 13 % per decade over the age of 45.</div>
<div type="abstract">The hypothesis has been put forward that the significant increase of incidence of depression in the elderly, the age‐dependent decline in male sexual vigour and the frequent appearance of parkinsonian symptoms in the later decades of life might be attributed to a decrease of dopamine and ‘trace amines’ in the brain. The possibility of countering these biochemical lesions of ageing by long‐term administration of deprenyl, a selective inhibitor of MAO‐B which facilitates dopaminergic and ‘trace‐aminergic’ activity in the brain, and is a safe drug in man, is considered in detail.</div>
</front>
</TEI>
<affiliations><list><country><li>Hongrie</li>
</country>
<region><li>Hongrie centrale</li>
</region>
<settlement><li>Budapest</li>
</settlement>
</list>
<tree><country name="Hongrie"><region name="Hongrie centrale"><name sortKey="Knoll, J" sort="Knoll, J" uniqKey="Knoll J" first="J." last="Knoll">J. Knoll</name>
</region>
<name sortKey="Knoll, J" sort="Knoll, J" uniqKey="Knoll J" first="J." last="Knoll">J. Knoll</name>
</country>
</tree>
</affiliations>
</record>

Pour manipuler ce document sous Unix (Dilib)

EXPLOR_STEP=$WICRI_ROOT/Wicri/Psychologie/explor/BernheimV1/Data/Main/Exploration

HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 000C81 | SxmlIndent | more

HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 000C81 | SxmlIndent | more

Pour mettre un lien sur cette page dans le réseau Wicri

{{Explor lien
   |wiki=    Wicri/Psychologie
   |area=    BernheimV1
   |flux=    Main
   |étape=   Exploration
   |type=    RBID
   |clé=     ISTEX:960D57F059B0F695D1B886989BE8CA37D6F1BFB5
   |texte=   Deprenyl (selegiline): the history of its development and pharmacological action
}}

This area was generated with Dilib version V0.6.33.
Data generation: Mon Mar 5 17:33:33 2018. Site generation: Thu Apr 29 15:49:51 2021

	Serveur d'exploration Hippolyte Bernheim
	Attention, ce site est en cours de développement ! Attention, site généré par des moyens informatiques à partir de corpus bruts. Les informations ne sont donc pas validées.

Serveur d'exploration Hippolyte Bernheim

Deprenyl (selegiline): the history of its development and pharmacological action

Deprenyl (selegiline): the history of its development and pharmacological action

Source :

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri