Current Medicinal Chemistry - Volume 21, Issue 1, 2014

The number of Asialoglycoprotein (ASGP) receptors on the hepatocytes of patients with liver disease is reduced and is thus considered a good indicator for the evaluation of liver function. ASGP receptor-targeted radiopharmaceuticals permit a non-invasive way to evaluate total and regional hepatic function and hepatic functional reserve visually and quantitatively. Over the past three decades, a variety of ASGP receptor-targ Read More

Glucose is an important molecule for metabolism. It is more actively taken up in tumor cells than in normal cells, thus making it possible to detect the tumor. Radiolabeled glucose derivates have been successfully employed for tumor imaging for several decades. This review focuses on the development of various radiolabeled glucose derivatives as tumor imaging probes with single photon emission computed tomography (S Read More

It is widely accepted that sigma ( σ) receptors represent a new and different avenue in the possible pharmacological treatment of cancer and several brain-related disorders. Of the two different σ receptor types the σ1 receptors are assumed to be of major impact for brain diseases. Molecular imaging of brain σ1 receptors with positron emission tomography (PET) or single photon emission computed tomography (SPE Read More

Serotonin and its various receptors are involved in numerous brain functions and neuropsychiatric disorders. The 5-HT1A family is the best characterized subtype of the fourteen currently known 5-HT receptors. The 5-HT1A receptor is closely involved in the pathogenesis of anxiety, depression, epilepsy and eating disorders and therefore is an important target for drug therapy. The development in the 1980s of molec Read More

The deposition of β-amyloid (Aβ) plaques in the parenchymal and cortical brain is accepted as the main pathological hallmark of Alzheimer’s disease (AD). According to the amyloid cascade hypothesis, the Aβ deposition in the brain appears to be a good diagnostic biomarker for AD and may also be a good predictive biomarker of this disease. Molecular imaging of Aβ plaques in the brain with positron emission tomograph Read More

The metabotropic glutamate 1 receptors (mGluR1) have been shown to play a role in neuropathic pain and neurological and psychiatric disorders such as ischemia, epilepsy, anxiety, as well as schizophrenia and other cognitionrelated disorders. As a result, mGluR1 has been an important target for drug development. As a radiotracer-based in vivo imaging technique Positron Emission Tomography (PET) is an important tool Read More

Nanoparticles can be near infrared (NIR)-fluorescent (e.g., gold nanoparticles, quantum dots or carbon nanotubes) or can have magnetic properties (e.g., iron oxide nanoparticles). These optical or magnetic properties can be exploited for use in thermal therapy and molecular imaging. Radiolabeled nanoparticles have proven to be promising tools in the diagnosis and therapy of malignant processes due to their multivale Read More

A series of radiolabeled peptides have been designed and optimized for tumor-targeted peptide receptor radionuclide therapy (PRRT). Pre-clinical and clinical applications of PRRT have shown promising results on tumor response, overall survival, and quality of life in patients with several kinds of tumors. 90Y-DOTA-TOC and 177Lu-DOTA-TATE are two of the most common radiopharmaceuticals with symptomatic improvements a Read More