5-HT7 receptor modulators: Amino groups attached to biphenyl scaffold determine functional activity was written by Kim, Youngjae;Park, Hyeri;Lee, Jeongeun;Tae, Jinsung;Kim, Hak Joong;Min, Sun-Joon;Rhim, Hyewhon;Choo, Hyunah. And the article was included in European Journal of Medicinal Chemistry in 2016.Product Details of 2314-37-6 This article mentions the following:
A novel scaffold for 5-HT7R modulators, a series of biphenyl-3-yl-methanamine derivatives with various amino groups I (R1 = H, Cl, Me, OMe; NR2R3 = 4-(2-methoxyphenyl)piperazine, 4-methyl-piperidine, NMe2, NMe), II (NR2R3 = 4-(2-methoxyphenyl)piperazine, 4-methyl-piperidine, NMe2, NMe) were designed and prepared Evaluation of functional activities as well as binding affinities of the title compounds identified partial agonists (EC50 = 0.55-3.2 μM) and full antagonists (IC50 = 5.57-23.1 μM) depending on the amino substituents. Mol. docking study suggested that the ligand-based switch in functional activity from agonist to antagonist results from the size of the amino groups and thereby different binding modes to 5-HT7R. In particular, interaction of the ligand with Arg367 of 5-HT7R is shown to differentiate agonists and antagonists. In the pharmacophore model study, two distinct pharmacophore models can tell whether a ligand is an agonist or an antagonist. Taken together, this study provides valuable information for designing novel compounds with selective agonistic or antagonistic properties against 5-HT7R. In the experiment, the researchers used many compounds, for example, 3-Iodo-4-methoxybenzaldehyde (cas: 2314-37-6Product Details of 2314-37-6).
3-Iodo-4-methoxybenzaldehyde (cas: 2314-37-6) belongs to iodide derivatives. Generally organic iodides can be divided into two classes of alkyl iodides and aryl iodides. Typical reactions of alkyl iodides include nucleophilic substitution, elimination, reduction, and the formation of organometallics. The C–I bond is the weakest of the carbon–halogen bonds. These bond strengths correlate with the electronegativity of the halogen, decreasing in the order F > Cl > Br > I. This periodic order also follows the atomic radius of halogens and the length of the carbon-halogen bond.Product Details of 2314-37-6
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com