AI Article Synopsis
- The study investigates the structure-activity relationship of potent ergoline compounds that selectively inhibit the CXCR3 receptor, achieving IC(50) values under 10nM in specific assays.
- Introduction of polar substituents improved activity in receptor occupancy assays, leading to more effective compounds.
- Compound 11a emerged as a particularly promising candidate due to its favorable pharmacokinetics and cross-reactivity with rodent CXCR3, which could be useful in animal studies.
Article Abstract
The structure-activity relationship of highly potent special ergolines which selectively block the chemokine receptor CXCR3 is reported. The most potent compounds showed IC(50) values below 10nM in both ligand binding and Ca(2+)-mobilization assays. However, these compounds were poorly active in an assay that measures receptor occupancy in blood. Introduction of polar substituents led to derivatives with IC(50) values below 10nM in this assay. Among them was compound 11a which showed both a favorable PK profile and cross reactivity with rodent CXCR3 making it a promising tool compound to further explore the role of CXCR3 in animal models.
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| http://dx.doi.org/10.1016/j.bmcl.2011.06.070 | DOI Listing |
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