Track topics on Twitter Track topics that are important to you
The latest addition to the serotonin (5-HT) receptor family is the 5-HT7 receptor (5-HT7R). This receptor has gained interest as a drug target due to its involvement in various disorders such as depression or schizophrenia. There is currently no clinically validated positron emission tomography (PET) tracer for the 5-HT7R available. But, the (arylpiperazinyl-butyl)oxindole scaffold provides a promising lead structure for this purpose. Here, we synthesized 12 (arylpiperazinyl-butyl)oxindole derivatives and in vitro affinity screening identified two structures with suitable affinity and selectivity to be radiolabelled and tested as 5-HT7R selective PET tracers. Next, the radiolabelled products [18F]ENL09 and [18F]ENL10 were evaluated as PET tracers in rats. Both tracers were found to be P-gp substrates but after P-gp inhibition, the brain uptake showed a regional distribution in line with the known 5-HT7R distribution and [18F]ENL10 brain binding was displaceable with a 5-HT7R selective ligand, whereas [18F]ENL09 was not. We find that [18F]ENL10 is a promising 5-HT7R selective PET tracer candidate that should be investigated in higher species.
This article was published in the following journal.
Name: ACS chemical neuroscience
Nuclear medicine has been implicated in the diagnosis and treatment of endocrine disorders for several decades. With recent development of PET tracers, functional imaging now plays a major role in end...
The nociceptin/orphanin FQ peptide (NOP) receptor-related ligands have been demonstrated in preclinical studies for several therapeutic applications. This article highlights (1) how nonhuman primates ...
The treatment of cancer remains a major challenge, especially after tumour cell dissemination and metastases formation. Expression of the urokinase-type plasminogen activation system including urokina...
Prostate cancer (PCa) is the most frequently diagnosed male malignant tumor and remains the second leading cause of male cancer mortality in the western countries. The second-generation antiandrogen e...
First clinical indications of positron emission tomography (PET) were in the fields of neurology and cardiology, but oncology is the domain in which PET got its recognition as an essential diagnostic ...
The goal of the current study is to evaluate the potential of the selected PET tracers to detect sarcoidotic lesions in lungs. The tracers are already in clinical use for the detection of ...
Background: Pituitary adenomas affect 10% of the population. Surgery offers the most cost-effective treatment modality but cure rates are only 40-70%, in part due to the limitations of Mag...
In this study we are looking at the blood flow to the heart using two different chemical tags or tracers that give off a low level of radiation. The tracers used in this study are called O...
This study is designed to obtain basic information on three PET imaging tracers developed to detect tau pathology in the brain. In this study, healthy control participants and participants...
PET/MRI (positron emission tomography/magnetic resonance imaging) with somatostatin analog tracers has the potential to provide an imaging technique targeting subclinical granulomatous dis...
Development of a library collection, including the determination and coordination of selection policy, assessment of needs of users and potential users, collection use studies, collection evaluation, identification of collection needs, selection of materials, planning for resource sharing, collection maintenance and weeding, and budgeting.
A TIE receptor found predominantly on ENDOTHELIAL CELLS. It is considered essential for vascular development and can form a heterodimer with the TIE-2 RECEPTOR. The TIE-1 receptor may play a role in regulating BLOOD VESSEL stability and maturation.
Radioactive substances added in minute amounts to the reacting elements or compounds in a chemical process and traced through the process by appropriate detection methods, e.g., Geiger counter. Compounds containing tracers are often said to be tagged or labeled. (Hawley's Condensed Chemical Dictionary, 12th ed)
Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.
Studies determining the effectiveness or value of processes, personnel, and equipment, or the material on conducting such studies. For drugs and devices, CLINICAL TRIALS AS TOPIC; DRUG EVALUATION; and DRUG EVALUATION, PRECLINICAL are available.
Selective serotonin reuptake inhibitors SSRIs
Serotonin and norepinephrine reuptake inhibitors (SNRIs) are a class of medications that are effective at easing depression symptoms. SNRIs are also sometimes used to treat other conditions such as anxiety and nerve pain. How SNRIs work Serotonin (se...
Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...
Psychiatry is the study of mental disorders and their diagnosis, management and prevention. Conditions include schizophrenia, severe depression and panic disorders among others. There are pharmaceutical treatments as well as other therapies to help...