Molecules, Vol. 24, Pages 3808: Synthesis of Novel Nicotinic Ligands with Multimodal Action: Targeting Acetylcholine α4β2, Dopamine and Serotonin Transporters
Molecules, Vol. 24, Pages 3808: Synthesis of Novel Nicotinic Ligands with Multimodal Action: Targeting Acetylcholine α4β2, Dopamine and Serotonin Transporters
Molecules doi: 10.3390/molecules24203808
Authors:
Juan Pablo González-Gutiérrez
Hernán Armando Pessoa-Mahana
Patricio Ernesto Iturriaga-Vásquez
Miguel Iván Reyes-Parada
Nicolas Esteban Guerra-Díaz
Martin Hodar-Salazar
Franco Viscarra
Pablo Paillali
Gabriel Núñez-Vivanco
Marcos Antonio Lorca-Carvajal
Jaime Mella-Raipán
María Carolina Zúñiga
Nicotinic acetylcholine receptors (nAChRs), serotonin transporters (SERT) and dopamine transporters (DAT) represent targets for the development of novel nicotinic derivatives acting as multiligands associated with different health conditions, such as depressive, anxiety and addiction disorders. In the present work, a series of functionalized esters structurally related to acetylcholine and nicotine were synthesized and pharmacologically assayed with respect to these targets. The synthesized compounds were studied in radioligand binding assays at α4β2 nAChR, h-SERT and h-DAT. SERT experiments showed not radioligand [3H]-paroxetine displacement, but rather an increase in the radioligand binding percentage at the central binding site was observed. Compound 20 showed Ki values of 1.008 ± 0.230 μM for h-DAT and 0.031 ± 0.006 μM for α4β2 nAChR...
Source: Molecules - Category: Chemistry Authors: Juan Pablo Gonz ález-Gutiérrez Hern án Armando Pessoa-Mahana Patricio Ernesto Iturriaga-V ásquez Miguel Iv án Reyes-Parada Nicolas Esteban Guerra-D íaz Martin Hodar-Salazar Franco Viscarra Pablo Paillali Gabriel N úñez-Vivanco Marcos Antonio Lorca Tags: Article Source Type: research