Arylpiperazine derivatives acting at 5-HT(1A) receptors.
Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT(1A) subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind 5-HT(1A)R sites. Among these, arylpiperazine derivatives represent one of the most important classes of 5-HT(1A)R ligands. This article will review the development of arylpiperazine derivatives acting at 5-HT(1A)Rs with an emphasis on structure-affinity relationships of agonists and antagonists, ligand-receptor interactions and pharmacological applications.
López-Rodríguez
M L
ML
Departamento de Química Orgánica I, Facultad de Ciencias Químicas, Universidad Complutense, Madrid, E-28040, Spain. mluzlr@ucmail.ucm.es
Ayala
D
D
Benhamú
B
B
Morcillo
M J
MJ
Viso
A
A
D001007:Anxiety / Q000188:drug therapy; D003863:Depression / Q000188:drug therapy; D008024:Ligands; D010879:Piperazines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D021281:Quantitative Structure-Activity Relationship; D011985:Receptors, Serotonin / Q000378:metabolism*; D044263:Receptors, Serotonin, 5-HT1; D012559:Schizophrenia / Q000188:drug therapy; D012702:Serotonin Antagonists / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D017366:Serotonin Receptor Agonists / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use
D008024:Ligands; D010879:Piperazines; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists