ICYP: A POTENTIAL PROLACTINOMA IMAGING AGENT

拟议的计划是评估125 I-碘氰基吲哚酚（ICYP）作为 可能是催乳素瘤的显像剂 泌乳素瘤是一种影响 约占闭经妇女的25%。 特异性泌乳素瘤成像， (1)允许早期检测，（2）提高诊断精度，和（3） 允许对药物治疗进行系列评估。 在初步研究中， 已经评估了D2受体拮抗剂螺哌利多的成像作用 剂 以前的工作集中在使用内源性抑制， 催乳素（PRL）释放作为一种成像手段。 现时的建议 重点是使用PRL释放的内源性刺激作为可能的 成像目标。 选择ICYP进行初步评估是基于其 对β肾上腺素能受体的高亲和力，涉及刺激 PRL释放 该提案详细介绍了几项旨在允许 评估成像潜力。 这些实验包括：（1） 正常和肿瘤诱导的初步组织分布研究 大鼠垂体组织，（2）β肾上腺素能受体的定量 在正常和肿瘤诱导的垂体中的数量，（3）确定 与D2受体相关的摄取程度，以及（4）竞争 使用体外模型的研究。 这些实验的方案是 包括.

The proposed plan is an evaluation of 125I-iodocyanopindolol (ICYP) as a possible prolactinoma imaging agent. Prolactinomas are tumors affecting about 25% of all women with amenorrhea. Specific prolactinoma imaging may, (1) permit earlier detection, (2) increase diagnostic precision, and (3) permit serial assessment of medical therapy. In preliminary studies we have evaluated a D2 receptor antagonist, spiroperidol, as an imaging agent. This previous work focused on use of the endogenous inhibition of prolactin (PRL) release as a means of imaging. The present proposal focuses on use of the endogenous stimulation of PRL release as a possible target for imaging. ICYP was selected for initial evaluation based on its high affinity for the Beta adrenergic receptor implicated in stimulation of PRL release. The proposal details several experiments designed to permit assessment of imaging potentials. These experiments include: (1) preliminary tissue distribution studies in both normal and tumor-induced rat pituitary tissue, (2) quantification of Beta adrenergic receptor numbers in both normal and tumor-induced pituitaries, (3) determination of the degree of uptake associated with the D2 receptor, and (4) competition studies using an in vitro model. Protocols for these experiments are included.