In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Synthesis and pharmacological evaluation of a new series of radiolabeled ligands for 5-HT7 receptor PET neuroimaging, published in 2014-04-30, which mentions a compound: 83435-58-9, mainly applied to PET imaging 5HT7 receptor radiotracer; 5-HT(7); Fluorine-18; PET; Positron emission tomography; Serotonin, Related Products of 83435-58-9.
The brain serotonin-7 receptor (5-HT7) is the most recently discovered serotonin receptor. It is targeted by several drug-candidates in psychopharmacol. and neuropharmacol. In these fields, positron emission tomog. (PET) is a mol. imaging modality offering great promise for accelerating the development process from preclin. discovery to clin. phases. We recently described fluorinated 5-HT7 radioligands, inspired by the structure of SB269970, the prototypical 5-HT7 antagonist. Although these results were promising, it appeared that the radiotracer-candidates suffered, among other drawbacks, from too low a 5-HT7 receptor affinity. In the present study, seven structural analogs of SB269970 were synthesized using design strategies aiming to improve their radiopharmacol. properties. Their 5-HT7 binding properties were investigated by cellular functional assay. The nitro-precursors of the analogs were radiolabeled by [18 F-]nucleophilic substitution, and in vitro autoradiog. was performed in rat brain, followed by in vivo microPET. The chem. and radiochem. purity of the fluorine radiotracers was > 99% with specific activity in the 40-129 GBq/μmol range. The seven derivatives presented heterogeneous binding affinities toward 5-HT7 and 5-HT1A receptors. While [18 F]2F3P3 had promising characteristics in vitro, it showed poor brain penetration in vivo, partially reversed after pharmacol. inhibition of P-glycoprotein. These results indicated that, while chem. modification of these series improved several radiotracer-candidates in terms of 5-HT7 receptor affinity and specificity toward 5-HT1A receptors, other physicochem. modulations would be required in order to increase brain penetration.
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Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica