Leopoldo, Marcello published the artcileStructure-Affinity Relationship Study on N-(1,2,3,4-Tetrahydronaphthalen-1-yl)-4-Aryl-1-Piperazinealkylamides, a New Class of 5-Hydroxytryptamine7 Receptor Agents, Application of 1-(3-Cyanophenyl)piperazine, the publication is Journal of Medicinal Chemistry (2004), 47(26), 6616-6624, database is CAplus and MEDLINE.
A series of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides I (n = 3-5, R1 = OMe, H, R2 = OMe, CN, Ac, SMe, OH, etc.) was prepared and their affinity for serotonin (5-hydroxytryptamine, 5-HT) 5-HT7, 5-HT1A, and 5-HT2A receptors was measured by in vitro binding assays. In relation to 5-HT7 receptor affinity, receptor binding studies indicated that (i) the optimal alkyl chain length was five methylenes, (ii) an unsubstituted 1,2,3,4-tetrahydronaphthalenyl nucleus was preferred, and (iii) the substitution pattern of the aryl ring linked to the piperazine ring played a crucial role. Several compound with high affinity for 5-HT7 receptors were identified. Among them, piperazinehexanamides I [n = 5, R1 = H, R2 = 2-OMe (II), 2-Ac (III), 2-SMe (IV), 2-OH (V), and 2-Me (VI)] were assayed for the 5-HT7 receptor-mediated relaxation of substance P-induced guinea pig ileum contraction. Compounds II, IV, and VI behaved as full agonists and compound III as a partial agonist, whereas derivative V acted as an antagonist. Among the compounds presented here, it emerged that IV was identified as a potent 5-HT7 receptor agonist (Ki = 0.22 nM, EC50 = 2.56 μM), endowed with selectivity over 5-HT1A and 5-HT2A receptors (200-fold and >1000-fold, resp.).
Journal of Medicinal Chemistry published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Application of 1-(3-Cyanophenyl)piperazine.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics