Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 83435-58-9, is researched, SMILESS is O=C(N1[C@@H](CO)CCC1)OC(C)(C)C, Molecular C10H19NO3Journal, ACS Omega called Synthesis, Radiolabeling, and in Vitro and in Vivo Evaluation of [18F]ENL30: A Potential PET Radiotracer for the 5-HT7 Receptor, Author is Tampio L’Estrade, Elina; Edgar, Fraser G.; Xiong, Mengfei; Shalgunov, Vladimir; Baerentzen, Simone L.; Erlandsson, Maria; Ohlsson, Tomas G.; Palner, Mikael; Knudsen, Gitte M.; Herth, Matthias M., the main research direction is PET radiotracer fluoride 18 ENL30 serotonin receptor S7.Category: thiazole.
The 5-HT7 receptor (5-HT7R) is involved in a broad range of physiol. conditions and disorders. Currently, there is no validated clin. positron emission tomog. (PET) tracer available; however, we have recently developed a promising 11C-labeled candidate. In this project, we aimed to further extend our efforts and develop an 18F-labeled derivative, coined [18F]ENL30. Fluorine-18 has several advantages over carbon-11 especially within the preclin. phase, where a long half-life usually increases evaluation throughput. ENL30 was successfully synthesized in a low albeit sufficient overall yield. Radiolabeling succeeded with a radiochem. yield of approx. 4.5%. Subsequent preclin. PET studies revealed that [18F]ENL30 binds specifically to the 5-HT7R but suffered from affinity to σ-receptors. Addnl., we identified [18F]ENL30 to be a P-gp substrate in rats. However, we believe that [18F]ENL30 may prove to be valuable in higher species that exhibit decreased P-gp dependency. If required, σ-receptor binding could, in such studies, be selectively blocked potentially allowing for selective 5-HT7R imaging.
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Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica