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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1997-4-11
pubmed:abstractText
1. Transcerebral microdialysis was used to monitor dopamine, 3,4-dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA) and trans-isomer of atypical neuroleptic drug carbidine concentrations in the dialysates from dorsal striatum of freely moving rats following i.p. administration of the drug at doses 0.5, 1,5 and 25 mg/kg. The changes in locomotor activity as well as catalepsy in rats following transcarbidine administration were also evaluated. 2. The microdialysis "point of no net flux" method was used to measure interstitial free concentration (IFC) of trans-carbidine in the dorsal striatum of freely moving rats following i.p. administration of the drug at dose 5 mg/kg. The maximal IFC of trans-carbidine was found to be approximately 1 mu M 20-40 min after injection. 3. The drug at doses up to 1 mg/kg produces elevation of dopamine release not affecting sufficiently its metabolite dialysate levels. IFC of the drug calculated for these doses will not exceed 0.24 pM. At the dose 5 mg/kg, i.p., elevation of both dopamine release and metabolism was observed and dopamine release increased slightly more than DOPAC dialysate levels. 4. Stimulatory action of trans-carbidine on locomotor activity of non-operated rats has been observed at doses 0.2 and 0.5 mg/kg, i.p.. 5. Only the dose 25 mg/kg of trans-carbidine (maximal calculated IFC 4.53 mu M) was found to be cataleptogenic. The drug at this dose failed to increase DA release but induced a marked increase of DOPAC and HVA output. 6. It is concluded that trans-carbidine in in vivo neurochemical and behavioural studies demonstrates the preferential antagonistic action on dopamine release-regulating autoreceptors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0278-5846
pubmed:author
pubmed:issnType
Print
pubmed:volume
20
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
291-305
pubmed:dateRevised
2009-11-3
pubmed:meshHeading
pubmed:year
1996
pubmed:articleTitle
Simultaneous monitoring of dopamine, its metabolites and trans-isomer of atypical neuroleptic drug carbidine concentrations in striatal dialysates of conscious rats.
pubmed:affiliation
Laboratory of Neurochemical Pharmacology, Institute of Pharmacology, Russian Academy of Medical Sciences, Moscow, Russia.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't