2019
DOI: 10.1016/j.bmcl.2019.126644
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Divalent cannabinoid-1 receptor ligands: A linker attachment point survey of SR141716A for development of high-affinity CB1R molecular probes

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Cited by 7 publications
(6 citation statements)
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“…A study in 2019 focusing on linker attachments of SR141716A suggested that C-5 of the pharmacophore was a suitable position for fluorescent moiety linkage. [155] A fluorescein fluorophore showed affinity to hCB 1 R at 260 AE 20 nM with a linker length of 12 atoms, suggesting the C-5 position can be utilised for high affinity CB 1 R probes.…”
Section: Fluorescent Pyrazole Derivativesmentioning
confidence: 98%
“…A study in 2019 focusing on linker attachments of SR141716A suggested that C-5 of the pharmacophore was a suitable position for fluorescent moiety linkage. [155] A fluorescein fluorophore showed affinity to hCB 1 R at 260 AE 20 nM with a linker length of 12 atoms, suggesting the C-5 position can be utilised for high affinity CB 1 R probes.…”
Section: Fluorescent Pyrazole Derivativesmentioning
confidence: 98%
“…Mixture of 5-and 6-isomer. (38). The Fmoc-protected amine (21b) (77.2 mg, 132.3 μmol) was dissolved in DCM (4.5 mL) before TFA (0.5 mL) was added.…”
Section: Tert-butyl (R)-(1-(5-(25-bis(trifluoromethyl)phenyl)-2-methy...mentioning
confidence: 99%
“…Moreover, T1117 binding to CB 1 R is sensitive to the allosteric ligand ORG27569 and thus it is applicable to the discovery of new allosteric drugs (Bruno et al, 2014). In 2009 a study carried out by Grant and co-workers focused on the CB 1 R inverse agonist SR141716A, established the C5 position of its central pyrazole ring as the optimal site for fluorescent moiety linkage (Grant et al, 2019). Thus, CB 1 R fluorescent probes (34-35, Figure 12) based on C5 conjugation of two SR141716A analogues with fluorescein isothiocyanate (FITC), were prepared.…”
Section: Fluorescent Probesmentioning
confidence: 99%