Structure-activity relationship studies of CNS agents, Part 32: Effect of structural modifications in 1-arylpiperazine derivatives on alpha(1) -adrenoreceptor affinity

• Published in: Archiv der Pharmazie (Weinheim) Vol. 330; no. 6; p. 177
• Main Authors: Mokrosz, M J, Paluchowska, M H, Charakchieva-Minol, S, Bień, A
• Format: Journal Article
• Language: English
• Published: Germany 01.06.1997
• Subjects: 8-Hydroxy-2-(di-n-propylamino)tetralin - metabolism; Adrenergic alpha-Agonists - chemical synthesis; Adrenergic alpha-Agonists - chemistry; Adrenergic alpha-Agonists - pharmacology; Animals; Brain - metabolism; Cerebral Cortex - metabolism; Hippocampus - metabolism; Kinetics; Piperazines - chemical synthesis; Piperazines - chemistry; Piperazines - pharmacology; Rats; Receptors, Adrenergic, alpha-1 - drug effects; Receptors, Adrenergic, alpha-1 - metabolism; Receptors, Serotonin - drug effects; Receptors, Serotonin - metabolism; Receptors, Serotonin, 5-HT1; Serotonin Receptor Agonists - chemical synthesis; Serotonin Receptor Agonists - chemistry; Serotonin Receptor Agonists - pharmacology; Structure-Activity Relationship
• ISSN: 0365-6233; 1521-4184

The alpha(1)-adrenergic and 5-HT1A serotonergic receptor affinities of a series of 1-arylpiperazines are presented. The role of the spacer and the influence of the terminal substituents on the alpha(1)-adrenoreceptor affinity and the 5-HT1A/alpha(1) receptor selectivity are discussed.