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 α1-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.
ChiDYKilbournMCKatzenellenbogenJAWelchMJ, (1987) A rapid and efficient method for the fluoroalkylation of amines and amides. Development of a method suitable for incorporation of the short-lived positron-emitting radionuclides F-18. J Org Chem52:658–661
4.
CoenenHHWienhardKStöcklinGLauferPHeboldIPawlikGHeissW-D, (1988) PET measurement of D2 and S2 receptorbinding of 3-N-(2-[F-18]fluoroethyl)spiperone in baboon brain. Eur J Nucl Med14:80–87
5.
HuangS-CBarrioJRHoffmanJMBahnMMSatyamurthyNPahlJJBaxterLRMazziottaJCPhelpsME, (1989) Kinetics of 3-(2′[18F]fluoroethyl)spiperone in human brain. J Cereb Blood Flow Metab9(suppl 1):S134
6.
JovkarSWienhardKPawlikGCoenenHH, (1989) The in vivo quantification of D2 dopamine and S2 serotonin receptor density and affinity in baboon brain with PET using 3-(2′-F-18)fluoroethylspiperone. J Cereb Blood Flow Metab9(suppl1):S194
7.
KiesewetterDOEckelmanWCCohenRMFinnRDLarsonSM, (1986) Syntheses and D2 receptor affinities of derivatives of spiperone containing aliphatic halogens. Appl Radiat Isot37:1181–1188
8.
LeysenJEGommerenWEensAde Chaffoy de CourcellesDStoofJCJanssenPAJ, (1988) Biochemical profile of risperidone, a new antipsychotic. J Pharmacol Exp Ther247:661–670
9.
LeysenJEGommerenWLaduronPM, (1978) Spiperone: A ligand of choice for neuroleptic receptors. Biochem Pharmacol27:307–316
10.
LyonRATitelerMFrostJJWhitehousePJWongDFWagnerHNDannalsRFLinksJMKuharMJ, (1986) 3H-3-N-Methylspiperone labels D2 Dopamine receptors in basal gauglia and S2 serotonin receptors in cerebral cortex. J Neurosci6:2941–2949
11.
WagnerHNJrBurnsHDDannalsRFWongDFLangstromBDuelferTFrostJJRavertHTLiksJMRosenbloomSBLukasSEKramerAVKuharME, (1983) Imaging dopamine receptors in the human brain by positron tomography. Science221:1264–1266
12.
WelchMJKatzenellenbogenJAMathiasCJBrodackJWCarlsonKEChiDYDenceCSKilbournMRPerlmutterJSRaichleMETer-PogossianMM, (1988) Nucl Med Biol15:83–97
13.
WienhardKCoenenHHPawlikGHeboldIJovkarSStöcklinGHeissW-D, (1989) PET investigations of the dopaminergic system in neurological patients using 3-N-[18F]-2-fluoroethyl)spiperone. In: Positron emission tomography in clinical research: Tracer modelling and radioreceptors (BeckersCGoffinetABolA, eds) Dordrecht: Kluver Acad. (in press)