Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors.
SAR around a known molecule with dual 5-HT(1D) antagonist and 5-HT(transporter) inhibitory activity has led to the discovery of molecules with improved dual activity and reduced cross-reactivity toward other aminergic receptors (5-HT(1B), alpha(1), and D(2)).
Bueno
Ana B
AB
Lilly SA, Avda. de la Industria, 30, 28108, Alcobendas, Madrid, Spain. bueno_ana_belen@lilly.com
Gilmore
Jeremy
J
Boot
John
J
Broadmore
Richard
R
Cooper
Jane
J
Findlay
Jeremy
J
Hayhurst
Lorna
L
Marcos
Alicia
A
Montero
Carlos
C
Mitchell
Stephen
S
Timms
Graham
G
Tomlinson
Rosemarie
R
Wallace
Louise
L
Walton
Leslie
L
D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D007700:Kinetics; D008956:Models, Chemical; D009281:Naphthalenes / Q000737:chemistry*; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology*; D044346:Receptor, Serotonin, 5-HT1D / Q000187:drug effects* / Q000378:metabolism; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000928:Antidepressive Agents; D009281:Naphthalenes; D010879:Piperazines; D044346:Receptor, Serotonin, 5-HT1D; D012702:Serotonin Antagonists; D017367:Selective Serotonin Reuptake Inhibitors