Publications by authors named "Rolf Baenteli"
Special ergolines efficiently inhibit the chemokine receptor CXCR3 in blood.
Bioorg Med Chem Lett
August 2011
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.
The special ergoline 1 is a highly potent, selective antagonist of the chemokine receptor CXCR3. The surprising selectivity of this LSD-related compound can be explained by different electronic and steric properties of the ergoline core structure caused by the urea portion of the molecule. Discovery, biopharmaceutical properties and first derivatives of this promising lead compound are discussed.
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