[¹⁸F]Fluspidine-A PET Tracer for Imaging of σ₁ Receptors in the Central Nervous System.

ABSTRACT: σ₁ receptors play a crucial role in various neurological and neurodegenerative diseases including pain, psychosis, Alzheimer's disease, and depression. Spirocyclic piperidines represent a promising class of potent σ₁ receptor ligands. The relationship between structural modifications and σ₁ receptor affinity and selectivity over σ₂ receptors led to the 2-fluoroethyl derivative fluspidine (2, K_i = 0.59 nM). Enantiomerically pure (S)-configured fluspidine ((S)-2) was prepared by the enantioselective reduction of the α,β-unsaturated ester 23 with NaBH₄ and the enantiomerically pure co-catalyst (S,S)-24. The pharmacokinetic properties of both fluspidine enantiomers (

SUBMITTER: Ludwig FA 

PROVIDER: S-EPMC10892410 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature