Quality Control of Boc-D-Prolinol. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: Boc-D-Prolinol, is researched, Molecular C10H19NO3, CAS is 83435-58-9, about Synthesis and Serotonergic Activity of 3-[2-(Pyrrolidin-1-yl)ethyl]indoles: Potent Agonists for the h5-HT1D Receptor with High Selectivity over the h5-HT1B Receptor. Author is Sternfeld, Francine; Guiblin, Alexander R.; Jelley, Richard A.; Matassa, Victor G.; Reeve, Austin J.; Hunt, Peter A.; Beer, Margaret S.; Heald, Anne; Stanton, Josephine A.; Sohal, Bindi; Watt, Alan P.; Street, Leslie J..
The design, synthesis, and biol. evaluation of a novel series of 3-[2-(pyrrolidin-1-yl)ethyl]indoles with excellent selectivity for h5-HT1D (formerly 5-HT1Dα) receptors over h5-HT1B (formerly 5-HT1Dβ) receptors are described. Clin. effective antimigraine drugs such as Sumatriptan show little selectivity between h5-HT1D and h5-HT1B receptors. The differential expression of h5-HT1D and h5-HT1B receptors in neural and vascular tissue prompted an investigation of whether a compound selective for the h5-HT1D subtype would have the same clin. efficacy but with reduced side effects. The pyrrolidine was initially identified as having 9-fold selectivity for h5-HT1D over h5-HT1B receptors. Substitution of the pyrrolidine ring with methylbenzylamine groups gave compounds with nanomolar affinity for the h5-HT1D receptor and 100-fold selectivity with respect to h5-HT1B receptors. Modification of the indole 5-substituent led to the oxazolidinones with ≤163-fold selectivity for the h5-HT1D subtype and improved selectivity over other serotonin receptors. The compounds were shown to be full agonists by measurement of agonist-induced [35S]GTPγS binding in CHO cells expressed with h5-HT receptors. This study suggests that the h5-HT1D and h5-HT1B receptors can be differentiated by appropriate substitution of the ligand in the region which binds to the aspartate residue and reveals a large binding pocket in the h5-HT1D receptor domain which is absent for the h5-HT1B receptor. The compounds described herein will be important tools to delineate the role of h5-HT1D receptors in migraine.
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Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica