In 2019.0 J MED CHEM published article about ACETYLCHOLINE-RECEPTORS; IN-VITRO; QUINOLINE DERIVATIVES; THERAPEUTIC TARGETS; LIGAND EFFICIENCY; FULL AGONIST; ALPHA-4-BETA-2; VARENICLINE; EPIBATIDINE; SUBTYPES in [Manetti, Dina; Bartolucci, Gianluca; Bellucci, Cristina; Chiaramonte, Niccolo; Dei, Silvia; Teodori, Elisabetta; Romanelli, Maria Novella] Univ Florence, Sect Pharmaceut & Nutraceut Sci, Dept Neurosci Psychol Drug Res & Childs Hlth NEUR, Via Ugo Schiff 6, I-50019 Sesto Fiorentino, Italy; [Garifulina, Alexandra; Spirova, Ekaterina; Shelukhina, Irina; Tsetlin, Victor] Russian Acad Sci, Shemyakin Ovchinnikov Inst Bioorgan Chem, Dept Mol Basis Neurosignaling, Miklukho Maklaya St 16-10, Moscow 117997, Russia; [Bazzicalupi, Carla] Univ Florence, Dept Chem Ugo Schiff, Via Lastruccia 3, I-50019 Sesto Fiorentino, Italy; [Mannelli, Lorenzo Di Cesare; Ghelardini, Carla] Univ Florence, Sect Pharmacol & Toxicol, Dept NEUROFARBA, Viale G Pieraccini 6, I-50139 Florence, Italy; [Gratteri, Paola] Univ Firenze, Lab Mol Modeling Cheminformat, Dept NEUROFARBA, Via Ugo Schiff 6, I-50019 Sesto Fiorentino, Italy; [Gratteri, Paola] Univ Firenze, QSAR, Via Ugo Schiff 6, I-50019 Sesto Fiorentino, Italy; [Varani, Katia] Univ Ferrara, Inst Pharmacol, Via Fossato di Mortara 17-19, I-44100 Ferrara, Italy in 2019.0, Cited 64.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Formula: C6H5NO
A three-dimensional database search has been applied to design a series of endo- and exo-3-(pyridin-3-yl)bicyclo[2.2.1]heptan-2-amines as nicotinic receptor ligands. The synthesized compounds were tested in radioligand binding assay on rat cortex against [H-3]-cytisine and [3H]-methyllycaconitine to measure their affinity for alpha 4 beta 2* and alpha 7* nicotinic receptors. The new derivatives showed some preference for the alpha 4 beta 2* over the alpha 7* subtype, with their affinity being dependent on the endo/exo isomerism and on the methylation degree of the basic nitrogen. The endo primary amines displayed the lowest K-i values on both receptor subtypes. Selected compounds (1a, 2a, 3a, and 6a) were tested on heterologously expressed alpha 4 beta 2, alpha 7, and alpha 3 beta 2 receptors and on SHSY-5Y cells. Compounds 1a and 2a showed alpha 4 beta 2 antagonistic properties while behaved as full agonists on recombinant alpha 7 and on SHSYSY cells. On the alpha 3 beta 2 subtype, only the chloro derivative 2a showed full agonist activity and submicromolar potency (EC50 = 0.43 mu M). The primary amines described here represent new chemotypes for the alpha 7 and alpha 3* receptor subtypes.
Formula: C6H5NO. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Manetti, D; Garifulina, A; Bartolucci, G; Bazzicalupi, C; Bellucci, C; Chiaramonte, N; Dei, S; Mannelli, LD; Ghelardini, C; Gratteri, P; Spirova, E; Shelukhina, I; Teodori, E; Varani, K; Tsetlin, V; Romanelli, MN or concate me.
Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem