In vitro and in vivo testing of the dopamine D1 ligand [123I]SCH 23982 with respect to its potential application in SPET investigations.
Nucl Med Biol
; 20(5): 607-16, 1993 Jul.
Article
in En
| MEDLINE
| ID: mdl-8358346
ABSTRACT
[123I]SCH 23982, a dopamine D1 ligand, was labelled in a large scale process and then tested in vitro for binding to rat brain sections and membranes. Because of the promising values of KD = 1.5 x 10(-10) M and Bmax = 0.7 x 10(-11) mol/g, in vivo evaluation was performed on rats and normal volunteers to test its possible usefulness for SPET imaging. In competition experiments, a higher binding in the presence of sulpiride was found while ketanserin displaced [123I]SCH 23982 only at a 10,000-fold excess. Differences between rats and men were seen with respect to their metabolism. SPET investigations failed because the washout of [123I]SCH 23982 was too rapid.
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Database:
MEDLINE
Main subject:
Benzazepines
/
Tomography, Emission-Computed, Single-Photon
/
Receptors, Dopamine D1
Limits:
Aged
/
Animals
/
Female
/
Humans
/
Male
/
Middle aged
Language:
En
Year:
1993
Type:
Article