Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
|
pubmed:dateCreated |
1989-7-21
|
pubmed:abstractText |
Rat neostriatal slices were superfused with medium containing 0.1 to 30 microM of the dopamine (DA)-releasing agent D-(+)-am-phetamine (AMPH) and the D-2 DA receptor antagonist (-)-sulpiride (10 microM) in the absence or presence of mu-, delta-, and kappa-selective opioids. AMPH dose-dependently enhanced the cyclic AMP production, as measured by its efflux from striatal slices, whereas simultaneous blockade of D-2 DA receptors by (-)-sulpiride strongly potentiated this effect. Both the mu-opioid receptor selective agonist [D-Ala2,MePhe4,Gly-ol5]enkephalin (0.01-3 microM) and the delta-opioid receptor selective agonist [D-Phe2-D-Pen5]enkephalin (DPDPE, 0.01-3 microM) inhibited the cyclic AMP efflux, stimulated by 10 microM AMPH in the presence of (-)-sulpiride, by 70 to 80%. The highly selective kappa-opioid receptor agonist U 50,488 (trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrol-idinyl)- cyclohexyl]benzeneacetamide methanesulfonate hydrate) (0.01-1 microM) had no effect. In contrast, the purported kappa-opioid receptor agonist bremazocine (3-300 nM) inhibited the stimulated adenylate cyclase activity to a similar extent as did [D-Ala2-MePhe4,Gly-ol5]enkephalin and DPDPE. Moreover, the selective irreversible delta-antagonist fentanyl isothiocyanate reversed both the inhibition caused by DPDPE and that caused by bremazocine, whereas the kappa-selective antagonist norbinaltorphimine showed no differences in its potency to antagonize the inhibitory effects of the different opioid agonists. The results indicate that opioids, by activating mu- or delta-, but not kappa-opioid receptors may cause a profound inhibition of adenylate cyclase activity stimulated by activation of (postsynaptic) D-1 DA receptors upon the (presynaptic) release of DA.(ABSTRACT TRUNCATED AT 250 WORDS)
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adenylate Cyclase,
http://linkedlifedata.com/resource/pubmed/chemical/Amphetamine,
http://linkedlifedata.com/resource/pubmed/chemical/Benzomorphans,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Morphinans,
http://linkedlifedata.com/resource/pubmed/chemical/Narcotics,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/bremazocine
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jun
|
pubmed:issn |
0022-3565
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
249
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
864-8
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:2543814-Adenylate Cyclase,
pubmed-meshheading:2543814-Amphetamine,
pubmed-meshheading:2543814-Animals,
pubmed-meshheading:2543814-Benzomorphans,
pubmed-meshheading:2543814-Corpus Striatum,
pubmed-meshheading:2543814-Cyclic AMP,
pubmed-meshheading:2543814-Dopamine,
pubmed-meshheading:2543814-Drug Interactions,
pubmed-meshheading:2543814-Male,
pubmed-meshheading:2543814-Morphinans,
pubmed-meshheading:2543814-Narcotics,
pubmed-meshheading:2543814-Rats,
pubmed-meshheading:2543814-Rats, Inbred Strains,
pubmed-meshheading:2543814-Receptors, Opioid
|
pubmed:year |
1989
|
pubmed:articleTitle |
Mu- and delta-opioid receptor-mediated inhibition of adenylate cyclase activity stimulated by released endogenous dopamine in rat neostriatal slices; demonstration of potent delta-agonist activity of bremazocine.
|
pubmed:affiliation |
Department of Pharmacology, Free University/Medical Faculty, Amsterdam, The Netherlands.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|