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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2
|
| pubmed:dateCreated |
1995-7-6
|
| pubmed:abstractText |
[11C]A-69024, (+/-)-1-(2-bromo-4,5-dimethoxybenzyl)-7-hydroxy-6-methoxy-2-[11C]methyl- 1,2,3,4-tetrahydroisoquinoline, is a specific and selective dopamine D1 radiotracer. The in vivo biodistribution of this novel radioligand in mice showed a high uptake in the striatum (6.7% ID/g) at 5 min, followed by clearance with a half-life of 16.1 min. As a measure of specificity, the striatal/cerebellar ratio reached a maximum of 7.4 at 30 min post-injection. Radioactivity in the striatum was reduced to the level of the cerebellum by pre-administration of the D1 antagonist SCH 23390 (1 mg/kg). Pretreatment of mice with spiperone (D2), 7-hydroxydipropylaminotetralin (7-OH-DPAT) (D3), clozapine (D4), ketanserin (5-HT2/5-HT2C), mazindol (monoamine reuptake), prazosin (alpha 1), and haloperidol (D2/sigma) had no inhibitory effect on [11C]A-69024 uptake in the striatum. The dextrorotatory enantiomer of the dopamine antagonist butaclamol inhibited striatal uptake, while the less active isomer (-)-butaclamol did not. [11C]A-69024 binding was inhibited by unlabeled A-69024 in a dose dependent manner (ED50 = 0.3 mg/kg) in the striatum while no change occurred in the cerebellum. [11C]A-69024 warrants further investigation as a PET ligand for examination of central dopamine D1 receptors in humans.
|
| pubmed:grant | |
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/A 69024,
http://linkedlifedata.com/resource/pubmed/chemical/Carbon Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Papaverine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine D1,
http://linkedlifedata.com/resource/pubmed/chemical/Tetrahydroisoquinolines
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Feb
|
| pubmed:issn |
0969-8051
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
22
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
221-6
|
| pubmed:dateRevised |
2007-11-14
|
| pubmed:meshHeading |
pubmed-meshheading:7767316-Analysis of Variance,
pubmed-meshheading:7767316-Animals,
pubmed-meshheading:7767316-Binding, Competitive,
pubmed-meshheading:7767316-Biological Transport,
pubmed-meshheading:7767316-Brain,
pubmed-meshheading:7767316-Carbon Radioisotopes,
pubmed-meshheading:7767316-Cerebellum,
pubmed-meshheading:7767316-Cerebral Cortex,
pubmed-meshheading:7767316-Corpus Striatum,
pubmed-meshheading:7767316-Kinetics,
pubmed-meshheading:7767316-Male,
pubmed-meshheading:7767316-Mice,
pubmed-meshheading:7767316-Mice, Inbred Strains,
pubmed-meshheading:7767316-Olfactory Bulb,
pubmed-meshheading:7767316-Papaverine,
pubmed-meshheading:7767316-Radioligand Assay,
pubmed-meshheading:7767316-Receptors, Dopamine D1,
pubmed-meshheading:7767316-Tetrahydroisoquinolines,
pubmed-meshheading:7767316-Tissue Distribution
|
| pubmed:year |
1995
|
| pubmed:articleTitle |
[11C]A-69024: a potent and selective non-benzazepine radiotracer for in vivo studies of dopamine D1 receptors.
|
| pubmed:affiliation |
Biomedicine and Health Program, Australia Nuclear Science and Technology Organisation, N.S.W., Sydney.
|
| pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.,
Research Support, U.S. Gov't, Non-P.H.S.
|