Beer H F, Lin S, Bläuenstein P, Hasler P, Schubiger P A, Maier A, Lichtensteiger W, Oettli R, Bekier A, Weder B
Division of Radiopharmacy, Paul Scherrer Institute, Villigen, Switzerland.
Nucl Med Biol. 1993 Jul;20(5):607-16. doi: 10.1016/0969-8051(93)90029-t.
[123I]SCH 23982, a dopamine D1 ligand, was labelled in a large scale process and then tested in vitro for binding to rat brain sections and membranes. Because of the promising values of KD = 1.5 x 10(-10) M and Bmax = 0.7 x 10(-11) mol/g, in vivo evaluation was performed on rats and normal volunteers to test its possible usefulness for SPET imaging. In competition experiments, a higher binding in the presence of sulpiride was found while ketanserin displaced [123I]SCH 23982 only at a 10,000-fold excess. Differences between rats and men were seen with respect to their metabolism. SPET investigations failed because the washout of [123I]SCH 23982 was too rapid.
多巴胺D1配体[123I] SCH 23982通过大规模方法进行标记，然后在体外测试其与大鼠脑切片和膜的结合情况。鉴于其解离常数KD = 1.5×10⁻¹⁰ M和最大结合容量Bmax = 0.7×10⁻¹¹ mol/g的良好数值，对大鼠和正常志愿者进行了体内评估，以测试其在单光子发射计算机断层显像（SPET）成像中的潜在用途。在竞争实验中，发现舒必利存在时结合率更高，而酮色林仅在过量10000倍时才能取代[123I] SCH 23982。在代谢方面观察到大鼠和人类之间存在差异。由于[123I] SCH 23982的洗脱太快，SPET研究未成功。
