High Occupancy of Sigma-1 Receptors in the Human Brain after Single Oral Administration of Fluvoxamine: A Positron Emission Tomography Study Using [11C]SA4503

@article{Ishikawa2007HighOO,
  title={High Occupancy of Sigma-1 Receptors in the Human Brain after Single Oral Administration of Fluvoxamine: A Positron Emission Tomography Study Using [11C]SA4503},
  author={Masatomo Ishikawa and Kiichi Ishiwata and Kenji Ishii and Yuichi Kimura and Muneyuki Sakata and Mika Naganawa and Kei-ichi Oda and Ryousuke Miyatake and Mihisa Fujisaki and Eiji Shimizu and Yukihiko Shirayama and Masaomi Iyo and Kenji Hashimoto},
  journal={Biological Psychiatry},
  year={2007},
  volume={62},
  pages={878-883}
}

High occupancy of sigma1 receptors in the human brain after single oral administration of donepezil: a positron emission tomography study using [11C]SA4503.

TLDR
It is demonstrated that donepezil binds to sigma1 receptors in the living human brain at therapeutic doses and sigma2 receptors may be implicated in the pharmacological mechanism ofdonepezil in the human brain.

High occupancy of s 1 receptors in the human brain after single oral administration of donepezil: a positron emission tomography

TLDR
It is demonstrated that donepezil binds to s1 receptors in the living human brain at therapeutic doses and may be implicated in the pharmacological mechanism ofdonepezil in the human brain.

Molecular imaging of σ receptors: synthesis and evaluation of the potent σ1 selective radioligand [18F]fluspidine

TLDR
The in vivo properties of [18F]fluspidine offer a high potential of this radiotracer for neuroimaging and quantitation of σ1 receptors in vivo and metabolic stability both in vitro and in animal experiments.

Roles of σ1 receptors in the mechanisms of action of CNS drugs

TLDR
Positron emission tomography with the σ1 specific ligand carbon-11-labelled 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine ([11C]SA4503) indicated that fluvoxamine and donepezil can bind to ρ1 receptors in the healthy human brain in a dose-dependent manner.

Sigma-1 Receptor Agonists and Their Clinical Implications in Neuropsychiatric Disorders.

TLDR
The role of s Sigma-1 receptors in the mechanistic action of some SSRIs, donepezil, neurosteroids, and ifenprodil, and the clinical implications for sigma-1 receptor agonists are discussed.

The role of sigma-1 receptors in the pathophysiology of neuropsychiatric diseases

TLDR
The function of sigma-1 receptors is reviewed and their role in the pathophysiology of neuropsychiatric diseases is attempted to be reinterpreted based on their new description as "receptor chaperones".

Positron Emission Tomography Imaging Evaluation of a Novel 18F-Labeled Sigma-1 Receptor Radioligand in Cynomolgus Monkeys.

TLDR
It is demonstrated that [18F]FBFP is a highly promising PET radioligand for imaging and quantification of σ1 receptors in humans.
...

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