[11C]SSR149415 的合成及正电子发射断层扫描初步成像研究。
Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography.
机构信息
Brookhaven National Laboratory, Medical Department, Upton, NY 11973, USA.
出版信息
Bioorg Med Chem Lett. 2010 May 15;20(10):3103-6. doi: 10.1016/j.bmcl.2010.03.108. Epub 2010 Apr 2.
SSR149415 was the first non-peptide vasopressin-(V(1b)) receptor antagonist reported. It has been used to probe the role of V(1b) receptors in animal models of depression, aggression, and stress-anxiety, and was progressed to clinical trials for the treatment of depression. Due to the interest in V(1b) receptors as a therapeutic target and the growing use of SSR149415 in preclinical research, we developed a method to label SSR145419 with carbon-11 and have studied its pharmacokinetics in non-human primates using positron emission tomography.
SSR149415 是第一个被报道的非肽血管加压素-(V(1b))受体拮抗剂。它已被用于在抑郁、攻击和应激-焦虑的动物模型中探测 V(1b)受体的作用，并已被推进到临床试验阶段，用于治疗抑郁症。由于对 V(1b)受体作为治疗靶点的兴趣以及 SSR149415 在临床前研究中的日益广泛应用，我们开发了一种用碳-11 标记 SSR145419 的方法，并使用正电子发射断层扫描研究了它在非人类灵长类动物中的药代动力学。
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