AI Article Synopsis
- Modification of a metabotropic glutamate receptor 2 negative allosteric modulator (mGluR NAM) resulted in new analogues with improved binding affinity and suitable properties for PET tracers.
- The new compounds displayed excellent lipophilicity and favorable physicochemical characteristics, making them promising candidates for imaging studies.
- C-MK-8056 was synthesized and showed the required affinity, selectivity, and properties to function effectively as a PET tracer for mGluR.
Article Abstract
Modification of potent, selective metabotropic glutamate receptor 2 negative allosteric modulator (mGluR NAM) led to a series of analogues with excellent binding affinity, lipophilicity, and suitable physicochemical properties for a PET tracer with convenient chemical handles for incorporation of a C or F radiolabel. [C]MK-8056 was synthesized and evaluated and demonstrated appropriate affinity, selectivity, and physicochemical properties to be used as a positron emission tomography tracer for mGluR.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10351059 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.3c00175 | DOI Listing |
Publication Analysis
Top Keywords
negative allosteric
8
physicochemical properties
8
discovery [c]mk-8056
4
[c]mk-8056 selective
4
selective pet
4
pet imaging
4
imaging agent
4
agent study
4
study mglur
4
mglur negative
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!