Ashworth S, Hume S P, Lammertsma A A, Opacka-Juffry J, Shah F, Pike V W
Cyclotron Unit, Royal Postgraduate Medical School, Hammersmith Hospital, London, UK.
Nucl Med Biol. 1996 Apr;23(3):245-50. doi: 10.1016/0969-8051(95)02053-5.
[3H]RP 62203 and [3H]SR 46349B binding were assessed in rat brain after intravenous (iv) injection. The distribution of specific binding of each radioligand corresponded to the known distribution of 5-HT2A receptor sites. The maximum signals (counts/g tissue over counts/g cerebellum) given by [3H]RP 62203 and [3H]SR 46349B were 9.0 +/- 0.9 at 60 min and 3.2 +/- 0.3 at 30 min, respectively, in frontopolar cortex. Specific binding was quantified using a reference-tissue compartment model. RP 62203 appears to be more suitable than SR 46349B for development as a PET radioligand on the basis of its higher receptor specific signal.
静脉注射后，在大鼠脑中评估了[3H]RP 62203和[3H]SR 46349B的结合情况。每种放射性配体的特异性结合分布与已知的5-HT2A受体位点分布相对应。在额极皮质中，[3H]RP 62203和[3H]SR 46349B在60分钟时给出的最大信号（每克组织计数除以每克小脑计数）分别为9.0±0.9，在30分钟时为3.2±0.3。使用参考组织室模型对特异性结合进行定量。基于其更高的受体特异性信号，RP 62203似乎比SR 46349B更适合作为PET放射性配体进行开发。
