6533b86ffe1ef96bd12cddcb

RESEARCH PRODUCT

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

Sung Won KimJacob M. HookerJacob M. HookerMatthias SchönbergerMatthias SchönbergerCarmine S. Leggett

subject

BiodistributionReceptors VasopressinIndolesPyrrolidinesmedicine.drug_classClinical BiochemistryPharmaceutical ScienceAnxietyBiochemistryPreclinical researchAnimal models of depressionDrug DiscoverymedicineAnimalsCarbon RadioisotopesReceptorMolecular Biologymedicine.diagnostic_testbusiness.industryChemistryDepressionOrganic ChemistryAntagonistReceptor antagonistClinical trialBiochemistryAnti-Anxiety AgentsPositron emission tomographyPositron-Emission TomographyMolecular MedicineNuclear medicinebusinessAntidiuretic Hormone Receptor AntagonistsPapio

description

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.

10.1016/j.bmcl.2010.03.108https://pubmed.ncbi.nlm.nih.gov/20400305