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In vivo binding of3H-N-methylspiperone to dopamine and serotonin receptors

Authors
Journal
Life Sciences
0024-3205
Publisher
Elsevier
Publication Date
Volume
40
Issue
10
Identifiers
DOI: 10.1016/0024-3205(87)90321-3

Abstract

Abstract 3H-N-methylspiperone ( 3H-NMSP) was used to label dopamine-2 and serotonin-2 in vivo in the mouse. The striatum/cerebellum binding ratio reached a maximum of 80 eight hours after intravenous administration of 3H-NMSP. The frontal cortex/cerebellum ratio was 5 one hour after injection. The binding of 3H-NMSP was saturable in the frontal cortex and cerebellum between doses of 10 and 1,000 ug/kg. Between 0.01 and 10 ug/kg the ratio total/nonspecific binding increased from 14 to 21. Inhibition of 3H-NMSP binding in the frontal cortex and striatum by ketanserin, a selective serotonin-2 antagonist, demonstrated that 20% of the total binding in the striatum was to serotonin-2 receptors and 91% of the total binding in the frontal cortex was to serotonin-2 receptors. Compared to 3H-spiperone, 3H-NMSP 1) results in a much higher specific/nonspecific binding ratio in the striatum and frontal cortex and 2) displays more than a two-fold higher brain uptake.

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