Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography.

Abstract SSR149415 was the first non-peptide vasopressin-(V1b) receptor antagonist reported. It has been used to probe the role of V1b 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 V1b 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.