N4-unsubstituted N1-arylpiperazines as high-affinity 5-HT1A receptor ligands
W Kuipers, I Van Wijngaarden, CG Kruse…
文献索引：Kuipers, Wilma; Wijngaarden, Ineke van; Kruse, Chris G.; Amstel, Marian ter Horst-van; Tulp, Martin Th. M.; IJzerman, Adriaan P. Journal of Medicinal Chemistry, 1995 , vol. 38, # 11 p. 1942 - 1954
In order to explore the structural requirements for high~-HT~ A affinity, a series of arylsubstituted W-phenylpiperazines were synthesized and evaluated for their ability to displace [3Hl-8-OH-DPAT from its specific binding sites in rat frontal cortex homogenates. We found 2-methoxy substitution to be favorable, while 4-methoxy substitution was detrimental for~-HT~ A affinity. Substitution with annelated rings at the 2, 3-positions was ...
