McN5652
McN5652' is a molecule of significant interest in the field of neuroimaging and neuroscience, particularly for its application in positron emission tomography (PET) studies as a radioligand. This compound can be radiolabeled, specifically with carbon-11 ([11C]), to create [11C]-(+)-McN5652, an enantiomer that exhibits high affinity for the serotonin transporter. The utilization of McN5652 in PET scans facilitates advanced research in molecular neuroimaging, allowing for detailed visualization of serotonin transporter distribution in the brain, as well as applications in lung imaging.
Pronunciation
Em-see-En-five-six-five-two
Development
Developed by McNeil Laboratories, a subsidiary of Johnson & Johnson, McN5652 was identified as one of the most potent serotonin reuptake inhibitors (SRI) at the time of its discovery, with sub-nanomolar inhibition constant (Ki) values indicating its high affinity and potency. Its development marked a significant step forward in the pharmacological characterization of SRIs and their potential diagnostic applications.
Pharmacodynamics
McN5652's binding affinity is not entirely selective to serotonin transporters; it also exhibits affinity for norepinephrine (NA) and dopamine (D) transporters, albeit to a lesser extent. The racemic mixture of McN5652 shows Ki values of 0.68 nM for 5-HT (serotonin), 2.9 nM for NA, and 36.8 nM for D transporters. The (+)-enantiomer specifically demonstrates a slightly higher affinity for the serotonin transporter (5-HT=0.39 nM), with NA=1.8 nM, and D=23.5 nM. These values highlight the compound's high but not exclusive affinity for serotonin transporters, compared to other SRIs like Paroxetine, which has been reported to have Ki values of 5-HT=0.44 nM, NA=20 nM, and DA=460 nM in studies by the same authors.
Applications in Neuroimaging
The radiolabeled form of McN5652, particularly the [11C]-(+)-McN5652 enantiomer, is used extensively in PET studies for its ability to bind specifically to serotonin transporters. This property makes it an invaluable tool in the investigation of serotonin's role in various neurological and psychiatric disorders, including depression, anxiety disorders, and schizophrenia. Additionally, its use extends to imaging studies of the lungs, showcasing its versatility as a radioligand.
Related Terms
- Serotonin Transporter
- Positron Emission Tomography
- Radioligand
- Neuroimaging
- Serotonin Reuptake Inhibitor
See Also
External links
- Medical encyclopedia article on McN5652
- Wikipedia's article - McN5652
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