In vitro pharmacological profile of 3-N-(2-fluoroethyl)spiperone.
The binding affinities of spiperone and 3-N-(2-fluoroethyl)spiperone (FESP) have been compared for several rodent brain receptor sites and for inhibition of monoamine release and uptake sites. FESP and spiperone have almost identical profiles, namely a high affinity for dopamine-D2 and serotonin-S2 receptors, a low affinity for alpha 1-adrenergic receptors, and negligible binding to other sites. These results suggest that available data on spiperone binding may be applied to the interpretation of PET data obtained with FESP.
Goffinet
A M
AM
Positron Tomography Laboratory, Louvain-la-Neuve, Belgium.
Leysen
J
J
Labar
D
D
D000818:Animals; D001921:Brain / Q000378:metabolism*; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D066298:In Vitro Techniques; D051381:Rats; D011954:Receptors, Dopamine / Q000378:metabolism; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin / Q000378:metabolism; D013134:Spiperone / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology
D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; C051175:3-N-(2-fluoroethyl)spiperone; D013134:Spiperone