Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

The discovery and development of a biological active molecule with therapeutic properties is an ever increasing complex task, highly unpredictable at the early stages and marked, in the end, by high rates of failure. As a consequence, the overall process leading to the production of a successful drug is very costly. The improvement of the net outcome in drug discovery and development would require, amongst other important factors, a good understanding of the molecular events that characterize the disease or pathology in order to better identify likely targets of interest, to optimize the interaction of an active agent (small molecule or macromolecule of natural or synthetic origin) with those targets, and to facilitate the study of the pharmacokinetics, pharmacodynamics and toxicity of an active agent in suitable models and in human subjects. The objective of this Research Topic is to highlight new developments and applications of imaging techniques with the objective of performing pharmacological studies in vivo, in animal models and in humans. In the domain of drug discovery, the pharmacological and biomedical questions constitute the center of attention. In this sense, it is fundamental to keep in mind the strengths and limitations of each analytical or imaging technique. At the end, the judicious application of the technique with the aim of supporting the search for answers to manifold questions arising during a long and painstaking path provides a continuous role for imaging within the complex area of drug discovery and development.

magnetic resonance imaging (MRI) --- computerized tomography(CT) --- positron emission tomography (PET) --- pharmacology --- single photon emission computed tomography (SPECT) --- imaging --- medical imaging --- ultrasound

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

Positron emission tomography (PET) and single-photon emission computed tomography (SPECT) are in vivo molecular imaging methods which are widely used in nuclear medicine for diagnosis and treatment follow-up of many major diseases. These methods use target-specific molecules as probes, which are labeled with radionuclides of short half-lives that are synthesized prior to the imaging studies. These probes are called radiopharmaceuticals. The use of PET and SPECT for brain imaging is of special significance since the brain controls all the body’s functions by processing information from the whole body and the outside world. It is the source of thoughts, intelligence, memory, speech, creativity, emotion, sensory functions, motion control, and other important body functions. Protected by the skull and the blood–brain barrier, the brain is somehow a privileged organ with regard to nutrient supply, immune response, and accessibility for diagnostic and therapeutic measures. Invasive procedures are rather limited for the latter purposes. Therefore, noninvasive imaging with PET and SPECT has gained high importance for a great variety of brain diseases, including neurodegenerative diseases, motor dysfunctions, stroke, epilepsy, psychiatric diseases, and brain tumors. This Special Issue focuses on radiolabeled molecules that are used for these purposes, with special emphasis on neurodegenerative diseases and brain tumors.

Research & information: general --- Biology, life sciences --- SV2A --- SV2B --- SV2C --- microPET --- [18F]UCB-H --- epilepsy --- PBIF --- distribution volume --- blocking assay --- preclinical imaging --- Alzheimer’s disease (AD) --- network measure --- graph theory --- brain network --- positron emission tomography (PET) --- persistent homology --- Phosphodiesterase 2A (PDE2A) --- Positron Emission Tomography (PET) --- Benzoimidazotriazine (BIT) --- fluorinated --- Mouse Liver Microsomes (MLM) --- cyclic nucleotide phosphodiesterase --- PDE2A radioligand --- nitro-precursor --- fluorine-18 --- in vitro autoradiography --- PET imaging --- opioid receptors --- positron emission tomography --- radiotracers --- μOR-, δOR-, κOR- and ORL1-ligands --- movement disorders --- pain --- drug dependence --- GBM --- biomarkers --- Sigma 1 --- Sigma 2 --- PD-L1 --- PARP --- IDH --- Alzheimer’s disease --- Parkinson’s disease --- β-amyloid plaques --- neurofibrillary tangles --- α-synucleinopathy --- diagnostic imaging probes --- orexin receptors --- PET --- radiotracer --- imaging --- alpha 7 --- nicotinic acetylcholine receptors --- nAChR --- autoradiography --- amino acid --- FET --- FACBC --- FDOPA --- immunoPET --- molecular imaging --- glioma --- brain metastases --- adenosine A2A receptor --- rotenone-based mouse model --- [18F]FESCH --- two-step one-pot radiosynthesis

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

Positron emission tomography (PET) and single-photon emission computed tomography (SPECT) are in vivo molecular imaging methods which are widely used in nuclear medicine for diagnosis and treatment follow-up of many major diseases. These methods use target-specific molecules as probes, which are labeled with radionuclides of short half-lives that are synthesized prior to the imaging studies. These probes are called radiopharmaceuticals. The use of PET and SPECT for brain imaging is of special significance since the brain controls all the body’s functions by processing information from the whole body and the outside world. It is the source of thoughts, intelligence, memory, speech, creativity, emotion, sensory functions, motion control, and other important body functions. Protected by the skull and the blood–brain barrier, the brain is somehow a privileged organ with regard to nutrient supply, immune response, and accessibility for diagnostic and therapeutic measures. Invasive procedures are rather limited for the latter purposes. Therefore, noninvasive imaging with PET and SPECT has gained high importance for a great variety of brain diseases, including neurodegenerative diseases, motor dysfunctions, stroke, epilepsy, psychiatric diseases, and brain tumors. This Special Issue focuses on radiolabeled molecules that are used for these purposes, with special emphasis on neurodegenerative diseases and brain tumors.

Research & information: general --- Biology, life sciences --- SV2A --- SV2B --- SV2C --- microPET --- [18F]UCB-H --- epilepsy --- PBIF --- distribution volume --- blocking assay --- preclinical imaging --- Alzheimer’s disease (AD) --- network measure --- graph theory --- brain network --- positron emission tomography (PET) --- persistent homology --- Phosphodiesterase 2A (PDE2A) --- Positron Emission Tomography (PET) --- Benzoimidazotriazine (BIT) --- fluorinated --- Mouse Liver Microsomes (MLM) --- cyclic nucleotide phosphodiesterase --- PDE2A radioligand --- nitro-precursor --- fluorine-18 --- in vitro autoradiography --- PET imaging --- opioid receptors --- positron emission tomography --- radiotracers --- μOR-, δOR-, κOR- and ORL1-ligands --- movement disorders --- pain --- drug dependence --- GBM --- biomarkers --- Sigma 1 --- Sigma 2 --- PD-L1 --- PARP --- IDH --- Alzheimer’s disease --- Parkinson’s disease --- β-amyloid plaques --- neurofibrillary tangles --- α-synucleinopathy --- diagnostic imaging probes --- orexin receptors --- PET --- radiotracer --- imaging --- alpha 7 --- nicotinic acetylcholine receptors --- nAChR --- autoradiography --- amino acid --- FET --- FACBC --- FDOPA --- immunoPET --- molecular imaging --- glioma --- brain metastases --- adenosine A2A receptor --- rotenone-based mouse model --- [18F]FESCH --- two-step one-pot radiosynthesis

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

Positron emission tomography (PET) is a very useful technique for medical diagnosis and drug development. Radiopharmaceuticals are a key element in PET techniques and one of the pivotal factors influencing the applications of PET. The aim of this Special Issue of Molecules is to report on the recent research work on a number of aspects of PET radiopharmaceuticals and their preclinical and clinical use. More specifically, the content of this Special Issue includes but is not limited to radiolabeling design, radiosynthesis, synthesis techniques, quality control methodologies, GMP production methods, product formulation, in vitro and in vivo preclinical PET evaluations, clinical evaluations, dosimetry, stability study and metabolite analysis, and modeling.

Medicine --- kinetic analysis --- Siglec-9 --- gallium-68 --- vascular adhesion protein --- VAP-1 --- infection --- inflammation --- osteomyelitis --- animal model --- Staphylococcus aureus --- multiple myeloma --- positron emission tomography/computed tomography --- radiopharmaceuticals --- 18F-fluorodeoxyglucose --- tetrazine ligation --- PET --- SPECT --- indium-11 --- fluorine-18 --- positron emission tomography (PET), defluorination --- isotopic exchange --- silicon-based fluoride acceptor --- bioorthogonal chemistry --- tetrazine --- inverse electron-demand Diels-Alder ligation --- opioid --- naloxone --- overdose --- fentanyl --- carfentanil --- [11C]carfentanil --- positron emission tomography --- receptor occupancy --- pharmacokinetics --- [18F]AlF --- NOTA --- NODAGA --- PODS --- thiol-reactive --- linker --- affibody molecule --- bioconjugation --- EGFR --- tumor imaging --- vulnerable plaque --- molecular imaging --- PET imaging --- nanobody --- single-domain antibody --- sub-millimetre resolution --- AlF-radiolabelling --- preclinical radiopharmaceutical dosimetry --- image-based internal dosimetry --- OLINDA --- MCT1/MCT4 lactate transporter inhibitor --- [18F]FACH --- radiation safety --- sigma-1 receptor availability --- orthotopic xenograft of glioblastoma in mouse --- small animal Positron Emission Tomography/Magnetic Resonance Imaging (PET/MRI) --- (S)-(−)-[18F]fluspidine --- imaging-based biomarker --- SV2A protein --- PET radiotracers --- synaptic loss --- radiochemistry --- preclinical development --- clinical outcomes --- monocarboxylate transporters (MCTs) --- FACH --- 18F-labeled analog of FACH --- α-CCA --- blood-brain barrier (BBB) --- positron emission tomography (PET) imaging --- peptides --- proteolysis --- metabolic stability

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

Radiopharmaceuticals are used in the diagnosis and treatment of various diseases, especially cancer. In general, radiopharmaceuticals are either salts of radionuclides or radionuclides bound to biologically active molecules, drugs, or cells. Tremendous progress has been made in discovering, developing, and commercializing numerous radiopharmaceuticals for the imaging and therapy of cancer. Significant research is ongoing in academia and the pharmaceutical industry to develop more novel radiolabeled compounds as potential radiopharmaceuticals for unmet needs. This Special Issue aims to focus on all aspects of the design, characterization, evaluation, and development of novel radiolabeled compounds for the diagnosis and treatment of cancer and the application of new radiochemistry and methodologies for the development of novel radiolabeled compounds. Outstanding contributions presented in this Special Issue will significantly add to the field of radiopharmaceuticals.

Research & information: general --- Chemistry --- positron emission tomography (PET) --- pyrazoles --- fluorine-18 --- radionuclides --- PET probes --- imaging pharmaceuticals --- hypopharyngeal cancer --- 188Re-liposome --- repeated therapy --- NGS --- microRNA --- aprepitant --- radiopharmaceuticals --- neurokinin 1 receptor antagonist --- radionuclide chelators --- kidney uptake --- cleavable linkers --- neutral endopeptidase (NEP) --- renal brush border enzymes --- prostate-specific membrane antigen (PSMA) --- cancer imaging and therapy --- somatostatin analogs --- radiolabeling --- radionuclide therapy --- imaging --- adrenergic receptor --- positron emission tomography --- radiotracer --- cholecystokinin-2 receptor --- minigastrin --- molecular imaging --- targeted radiotherapy --- lutetium-177 --- EpCAM --- radionuclide --- SPECT --- iodine --- PIB --- breast --- cancer --- PET --- target-specific biomolecules --- immunoPET imaging pharmaceuticals --- production processes --- 124I-labeled monoclonal antibodies --- radiotracers --- AAZTA --- scandium-44 --- FAP --- SA --- DPP --- PREP --- radioiodine labeling --- radioiodination --- biomolecules --- peptides --- proteins --- monoclonal antibodies --- 123,124,125,131I-labeled molecules and biomolecules --- n/a