and sigma 1 receptor imaging studies in different disease states.

The sigma receptor system has been classified into two distinct subtypes, sigma 1 (σ1R) and sigma 2 (σ2R). Sigma 1 receptors (σ1Rs) are involved in many neurodegenerative diseases and different central nervous system disorders such as Alzheimer's disease, Parkinson's disease, schizophrenia, and drug addiction, and pain. This makes them attractive targets for developing radioligands as tools to gain a better understanding of disease pathophysiology and clinical diagnosis.

Exploring 1-adamantanamine as an alternative amine moiety for metabolically labile azepane ring in newly synthesized benzo[]thiazol-2(3)one σ receptor ligands.

In this work we report the structure-activity relationships, binding properties, and metabolic stability studies of a series of benzo[]thiazol-2(3)one as sigma receptors (σRs) ligands. Specifically, to improve the metabolic stability of the cyclic amine fragment of our lead compound (), the metabolically unstable azepane ring was replaced with a 1-adatamantamine moiety. Within the synthesized analogs, compound had low nanomolar affinity for the σR ( = 7.