SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition.
In this paper, SLV310 is presented as a novel, potential antipsychotic displaying the interesting combination of potent dopamine D(2) receptor antagonism and serotonin reuptake receptor inhibition in one molecule. As such, SLV310 could be useful in treating a broad range of symptoms in schizophrenia. This paper describes the structure-activity relationship in a series of compounds leading to SLV310 (6b, 2-[4-[4-(5-fluoro-1H-indol-3-yl)-3,6-dihydro-2H-pyridin-1-yl]-butyl]-phthalimide) together with pharmacological data showing the unique profile of this compound.
van Hes
Rolf
R
Solvay Pharmaceuticals Research Laboratories, PO Box 900, 1380 BA Weesp, The Netherlands.
Smid
Pieter
P
Stroomer
Cees N J
CN
Tipker
Koos
K
Tulp
Martin Th M
MT
van der Heyden
Jan A M
JA
McCreary
Andrew C
AC
Hesselink
Mayke B
MB
Kruse
Chris G
CG
D006916:5-Hydroxytryptophan / Q000494:pharmacology; D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D001058:Apomorphine / Q000037:antagonists & inhibitors; D001522:Behavior, Animal / Q000187:drug effects; D016466:CHO Cells; D006224:Cricetinae; D018491:Dopamine Agonists / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000494:pharmacology*; D065127:Dopamine D2 Receptor Antagonists; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007202:Indicators and Reagents; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010797:Phthalimides / Q000138:chemical synthesis* / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D017367:Selective Serotonin Reuptake Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D006916:5-Hydroxytryptophan; D014150:Antipsychotic Agents; D001058:Apomorphine; D018491:Dopamine Agonists; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D007202:Indicators and Reagents; D010797:Phthalimides; D011725:Pyridines; D017367:Selective Serotonin Reuptake Inhibitors; C476321:2-(4-(4-(5-fluoro-1H-indol-3-yl)-3,6-dihydro-2H-pyridin-1-yl)butyl)-phthalimide