Moerlein S M, Perlmutter J S, Welch M J
Edward Mallinckrodt Institute of Radiology, St. Louis, MO 63110, USA.
Nucl Med Biol. 1995 Aug;22(6):809-15. doi: 10.1016/0969-8051(95)00022-p.
[18F]Benperidol ([18F]BP), a positron-emitting analogue of the dopaminergic D2 antagonist benperidol, was evaluated as a radiopharmaceutical for use with positron emission tomography (PET). PET imaging of baboons after i.v. injection of [18F]BP indicated that the radiofluorinated ligand rapidly localized in vivo within dopaminergic receptor-rich cerebral tissues, and that selective disposition was retained for over 2 h. Pretreatment of an animal with unlabeled receptor-specific antagonists prior to injection of [18F]BP confirmed that the radioligand bound specifically to central D2 receptors in vivo, and not to S2 or D1 receptors. [18F]BP bound to D2 receptors in a reversible manner; unlabeled eticlopride displaced D2 receptor-bound [18F]BP in vivo. The radioligand was metabolized in the periphery to polar metabolites which are not expected to cross the blood-brain barrier. [18F]BP has advantages over other tracers as a radiopharmaceutical for PET study of central D2 receptor activity, and can be applied for noninvasive evaluation of the interaction of unlabeled drugs with central D2 receptor sites.
[18F]苄哌利多（[18F]BP）是多巴胺能D2拮抗剂苄哌利多的正电子发射类似物，被评估作为一种用于正电子发射断层扫描（PET）的放射性药物。静脉注射[18F]BP后对狒狒进行PET成像显示，这种放射性氟化配体在体内迅速定位于富含多巴胺能受体的脑组织中，并且选择性分布保持超过2小时。在注射[18F]BP之前用未标记的受体特异性拮抗剂对动物进行预处理，证实了该放射性配体在体内特异性结合中枢D2受体，而非S2或D1受体。[18F]BP以可逆方式结合D2受体；未标记的依托必利在体内可取代与D2受体结合的[18F]BP。该放射性配体在外周代谢为极性代谢产物，预计不会穿过血脑屏障。作为用于PET研究中枢D2受体活性的放射性药物，[18F]BP比其他示踪剂具有优势，并且可用于无创评估未标记药物与中枢D2受体位点的相互作用。
