Gruber, Corinna G. and Pegoli, Andrea and Mueller, Christoph and Graetz, Lukas and She, Xueke and Keller, Max (2020) Differently fluorescence-labelled dibenzodiazepinone-type muscarinic acetylcholine receptor ligands with high M2R affinity. RSC MEDICINAL CHEMISTRY, 11 (7). pp. 823-832. ISSN , 2632-8682
Full text not available from this repository. (Request a copy)Abstract
A series of fluorescent dibenzodiazepinone-type muscarinic acetylcholine M(2)receptor (M2R) ligands was synthesized using various fluorescent dyes (5-TAMRA,lambda(ex)/lambda(em)approximate to 547/576 nm; BODIPY 630/650,lambda(ex)/lambda(em)approximate to 625/640 nm; pyridinium dye Py-1,lambda(ex)/lambda(em)approximate to 611/665 nm and pyridinium dye Py-5,lambda(ex)/lambda(em)approximate to 465/732 nm). All fluorescent probes exhibited high M2R affinity (pK(i)(radioligand competition binding): 8.75-9.62, pK(d)(flow cytometry): 8.36-9.19), a very low preference for the M2R over the M(1)and M(4)receptors and moderate to pronounced M2R selectivity compared to the M(3)and M(5)receptors. The presented fluorescent ligands are considered useful molecular tools for future studies using methods such as fluorescence anisotropy and BRET based MR binding assays.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | HISTAMINE H-2-RECEPTOR; NEUROPEPTIDE-Y; PHARMACOLOGICAL-ACTIVITY; MOLECULAR PROBES; GPCR LIGANDS; BINDING; DERIVATIVES; ANTAGONISTS; TOOLS; IDENTIFICATION; |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 19 Mar 2021 08:31 |
| Last Modified: | 19 Mar 2021 08:31 |
| URI: | https://pred.uni-regensburg.de/id/eprint/44280 |
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