Safety of tert-Butyl (5-aminopentyl)carbamateIn 2020 ,《Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu2/4 heterodimeric receptor results in a compound with mGlu2/2 homodimer selectivity》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Fulton, Mark G.; Loch, Matthew T.; Rodriguez, Alice L.; Lin, Xin; Javitch, Jonathan A.; Conn, P. Jeffrey; Niswender, Colleen M.; Lindsley, Craig W.. The article conveys some information:
This Letter details our ongoing efforts to develop selective pos. allosteric modulators (PAMs) of the mGlu2/4 heterodimeric receptor that exists in the CNS and may represent a novel drug target to modulate the glutamatergic system. As multiple hit-to-lead campaigns from HTS hits failed to produce selective small mol. mGlu2/4 heterodimer PAMs, we were inspired by the work of Portoghese to synthesize and evaluate a set of nine bivalent tethered ligands (possessing an mGlu2 PAM at one terminus and an mGlu4 PAM at the other). Utilizing G protein-Inwardly Rectifying Potassium (GIRK) channel functional assays, we found that the tethered ligands displayed PAM activity in a cell line co-expressing both mGlu2 and mGlu4 but also in cells expressing mGlu2 or mGlu4 alone. In a CODA-RET assay, one of the tethered ligands potentiated mGlu2/4 heterodimers; however, another compound displayed 75-fold preference for the mGlu2/2 homodimer over heterodimeric mGlu2/4 or homomeric mGlu4/4. This work highlights the development of mGlu receptor PAMs with homodimer/heterodimer preference and expands the potential for PAMs as tethered ligands beyond the more classical antagonists and NAMs. In the experimental materials used by the author, we found tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Safety of tert-Butyl (5-aminopentyl)carbamate)
Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Safety of tert-Butyl (5-aminopentyl)carbamate
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