Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
A series of serotonin 5-HT1B ligands were synthesized and evaluated for their potency and selectivity against other 5-HT receptor subtypes. Many of these new compounds displayed high affinity and selectivity for the 5-HT1B receptor and compound 6c was found to have the in vitro binding profile necessary for development as a PET radioligand.
Huang
Yiyun
Y
Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA. hh285@columbia.edu
Bae
Sung-A
SA
Roth
Bryan L
BL
Laruelle
Marc
M
D000577:Amides; D006801:Humans; D008024:Ligands; D010879:Piperazines; D011485:Protein Binding; D011869:Radioligand Assay; D044302:Receptor, Serotonin, 5-HT1B / Q000737:chemistry / Q000378:metabolism*; D018490:Serotonin Agents / Q000138:chemical synthesis* / Q000737:chemistry; D013329:Structure-Activity Relationship
D000577:Amides; D008024:Ligands; D010879:Piperazines; D044302:Receptor, Serotonin, 5-HT1B; D018490:Serotonin Agents; C031503:phenylpiperazine