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Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, causing turnover rates to depend strongly on interfacial structure and composition, 89343-06-6, Name is Ethynyltriisopropylsilane, SMILES is CC([Si](C(C)C)(C#C)C(C)C)C, in an article , author is Derkach, K., V, once mentioned of 89343-06-6, Quality Control of Ethynyltriisopropylsilane.
Low-Molecular-Weight Ligands of Luteinizing Hormone Receptor with Antagonistic Activity
Currently, a search for selective antagonists of luteinizing hormone (LH) receptor, which are necessary to suppress steroidogenesis in hormone-dependent tumors and to prevent the ovarian hyperstimulation syndrome, is carried out. One approach to solving this problem is the development of low-molecular-weight antagonists of the allosteric site of this receptor located in its transmembrane domain. The aim of this work was to develop the heterocyclic compounds, the derivatives of thieno[2,3-d]pyrimidine (TP31), pyrimido [4,5,6-de] [1,6]naphthyridine (PP10), and pyrido[3,4-d]pyrimidine (PP17), and to study their ability to influence the functional activity of the LH receptor in the in vitro and in vivo conditions. It was shown that at micromolar concentrations TP31 suppressed stimulating effects of human chorionic gonadotropin (hCG) on the adenylyl cyclase activity in rat testicular membranes. Yet more pronounced was the suppressing effect of TP31 on the stimulating effect of TP03, an allosteric agonist of the LH receptor. This was due to a higher selectivity of the TP31 antagonist with respect to the cAMP-dependent signaling cascades, predominantly activated by TP03 and realized through Gs proteins. PP17 inhibited stimulatory effects of hCG and TP03 on the adenylyl cyclase activity to a similar extent but was less potent than TP31. Upon intratesticular (10 mg/kg) or intraperitoneal (45 mg/kg) administration to male rats, TP31 and PP17 decreased the baseline plasma level of testosterone and inhibited the testosterone production stimulated by hCG (100 IU/rat); the inhibitory effect of TP31 was much more pronounced than that of PP17. PP10 exhibited a weaker antagonistic activity than TP31 and PP17 in the in vitro and in vivo conditions. The data obtained indicate that TP31, the most active functional antagonist among the studied compounds, by binding to the allosteric site of the LH receptor, makes it less accessible to allosteric agonists and impairs the hormonal signal transduction through the LH receptor. This suggests the prospects of the development of TP31-based inhibitors of LH-dependent pathways and steroidogenesis.
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Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem