Decades of study on the role of mitochondria in living cells have evidenced the importance of the 18 kDa mitochondrial translocator protein (TSPO), first discovered in the 1977 as an alternative binding site for the benzodiazepine diazepam in the kidneys. This protein participates in a variety of cellular functions, including cholesterol transport, steroid hormone synthesis, mitochondrial respi...

Microglial activation is a key pathological feature of Alzheimer's disease (AD). PET imaging of translocator protein 18 kDa (TSPO) is a strategy to detect microglial activation in vivo. Here we assessed flutriciclamide ([18F]GE-180), a new second-generation TSPO-PET radiotracer, for its ability to monitor response to LM11A-31, a novel AD therapeutic in clinical trials. AD mice displaying pathol...

A new fluorine-substituted ligand, compound 1 (CB251), with a very high affinity (Ki = 0.27 ± 0.09 nM) and selectivity for the 18-kDa translocator protein (TSPO), is presented as an attractive biomarker for the diagnosis of neuroinflammation, neurodegeneration and tumour progression. To test compound 1 as a TSPO PET imaging agent in vivo, 2-(2-(4-(2-[(18)F]fluoroethoxy)phenyl)-6,8-dichloroimida...

Atrial fibrillation is the most common arrhythmia encountered in clinical practice. It can cause severe complications such as congestive heart failure and stroke. However, identification of prime targets for efficient therapeutic intervention remains a challenge. In vitro rabbit heart models of ischemia-, stretch-, and cholinergic agitation-induced atrial fibrillation were developed, and pharma...

BACKGROUND We have previously shown that the anti-neoplastic agent erucylphosphohomocholine (ErPC3) requires the mitochondrial 18 kDa Translocator protein (TSPO), formerly known as the peripheral-type benzodiazepine receptor (PBR), to induce cell death via the mitochondrial apoptosis pathway. METHODS With the aid of the dye JC-1 and cyclosporin A, applied to glioblastoma cells, we now investi...

The 18 kDa translocator protein (TSPO) is an evolutionarily conserved transmembrane found embedded in the outer mitochondrial membrane. A secondary target for benzodiazepine diazepam, TSPO has been a of interest researchers decades, particularly owing to its well-established links inflammatory conditions central and peripheral nervous systems. It become key biomarker assessing microglial activa...

We examined the possibility of a differential spatial control in the endogenous production of 3alpha5alpha-reduced steroids and its consequences on GABA(A) receptor-mediated miniature IPSCs (mIPSCs) in laminas II and III-IV of the rat spinal cord dorsal horn (DH). Early in postnatal development [younger than postnatal day 8 (P8)], mIPSCs displayed slow decay kinetics in laminas II and III-IV re...

Contractile dysfunction and subsequent development of cardiomyopathies are well known limiting factors in the treatment of cancer with doxorubicin and have been linked to mitochondrial dysfunction. Here, using adult isolated paced cardiomyocytes, we have demonstrated that ligands of translocator protein (TSPO) 4'-chlorodiazepam and TRO40303 prevented the doxorubicin-induced alterations in contr...

This study investigated whether the second-generation translocator protein 18kDa (TSPO) radioligand, [18F]-FEPPA, could be used in neurodegenerative parkinsonian disorders as a biomarker for detecting neuroinflammation in the striatum. Neuroinflammation has been implicated as a potential mechanism for the progression of Parkinson's disease (PD). Positron Emission Tomography (PET) radioligand ta...