Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography.
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.
Schönberger
Matthias
M
Brookhaven National Laboratory, Medical Department, Upton, NY 11973, USA.
Leggett
Carmine
C
Kim
Sung Won
SW
Hooker
Jacob M
JM
D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D065092:Antidiuretic Hormone Receptor Antagonists; D001007:Anxiety / Q000188:drug therapy; D002250:Carbon Radioisotopes / Q000737:chemistry; D003863:Depression / Q000188:drug therapy; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D010215:Papio; D049268:Positron-Emission Tomography; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D017483:Receptors, Vasopressin / Q000378:metabolism
C456029:1-(5-chloro-1-((2,4-dimethoxyphenyl)sulfonyl)-3-(2-methoxyphenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl)-4-hydroxy-N,N-dimethyl-2-pyrrolidinecarboxamide; D014151:Anti-Anxiety Agents; D065092:Antidiuretic Hormone Receptor Antagonists; D002250:Carbon Radioisotopes; D007211:Indoles; D011759:Pyrrolidines; D017483:Receptors, Vasopressin