Linked Life Data

2572424

Source:http://linkedlifedata.com/resource/pubmed/id/2572424

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1989-12-1
pubmed:abstractText
The enantiomers of the potent and selective dopamine (DA) D-2 receptor agonist 2-(N-propyl-N-2-thienylethyl-amino)-5-hydroxytetralin, N-0437, were tested for their pharmacological actions on DA D-2 autoreceptors in vivo, by measuring DA release by microdialysis during local administration of both drugs and in vitro, by measuring their effects on the electrically stimulated release of [3H]DA from striatal slices. In both experimental situations (-)-N-0437, at low doses, acted as an agonist on receptors controlling DA release. However, in vivo at a concentration of 10 microM (-)-N-0437 induced a short-lasting increase in DA release and in vitro the inhibitory effect of (-)-N-0437 was significantly less pronounced at higher concentrations (1-10 microM). (+)-N-0437 (0.1-10 microM) showed an antagonistic action both in vivo and in vitro. Following inhibition of the neuronal impulse flow with tetrodotoxin, (+)-N-0437 failed to increase DA release suggesting the effect of this enantiomer is not associated with an amphetamine-like action on the nerve terminal. The use of the DA re-uptake inhibitor GBR 12909 confirmed the antagonism of (+)-N-0437 towards DA receptors. Since it is known that (+)-N-0437 acts as an agonist on DA D-2 autoreceptors controlling the synthesis of DA, these results provide additional evidence for the existence of distinct DA D-2 autoreceptor populations involved in the release and synthesis of DA. The differential actions of (-)- and (+)-N-0437 gave rise to mutual antagonism of the actions of the enantiomers both in vivo and in vitro, thus providing a strong argument for using the enantiomers instead of the racemate in clinical situations.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
4
pubmed:volume
166
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1-11
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed-meshheading:2572424-Animals, pubmed-meshheading:2572424-Apomorphine, pubmed-meshheading:2572424-Catheterization, pubmed-meshheading:2572424-Corpus Striatum, pubmed-meshheading:2572424-Dialysis, pubmed-meshheading:2572424-Dopamine, pubmed-meshheading:2572424-Dopamine Agents, pubmed-meshheading:2572424-Electric Stimulation, pubmed-meshheading:2572424-Kainic Acid, pubmed-meshheading:2572424-Male, pubmed-meshheading:2572424-Naphthalenes, pubmed-meshheading:2572424-Neurotransmitter Uptake Inhibitors, pubmed-meshheading:2572424-Piperazines, pubmed-meshheading:2572424-Rabbits, pubmed-meshheading:2572424-Rats, pubmed-meshheading:2572424-Rats, Inbred Strains, pubmed-meshheading:2572424-Stereoisomerism, pubmed-meshheading:2572424-Tetrahydronaphthalenes, pubmed-meshheading:2572424-Tetrodotoxin, pubmed-meshheading:2572424-Thiophenes, pubmed-meshheading:2572424-Time Factors
pubmed:year
1989
pubmed:articleTitle
The enantiomers of the dopamine agonist N-0437: in vivo and in vitro effects on the release of striatal dopamine.
pubmed:affiliation
Department of Pharmacy, State University of Groningen, The Netherlands.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't