Studies towards the next generation of antidepressants. Part 1: Indolylcyclohexylamines as potent serotonin reuptake inhibitors.
A series of indolylcyclohexylamines possessing potent and selective serotonin reuptake inhibition is reported. The most interesting compounds proved to have subnanomolar 5-HT transporter activity, and exhibited moderate 5-HT(1A) affinity.
Meagher
K L
KL
Global Chemical Sciences and Neuroscience Departments, Wyeth-Ayerst Research Laboratories, CN 8000, NJ 08543-8000, Princeton, USA.
Mewshaw
R E
RE
Evrard
D A
DA
Zhou
P
P
Smith
D L
DL
Scerni
R
R
Spangler
T
T
Abulhawa
S
S
Shi
X
X
Schechter
L E
LE
Andree
T H
TH
D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D016466:CHO Cells; D002352:Carrier Proteins / Q000187:drug effects* / Q000378:metabolism; D006224:Cricetinae; D003514:Cyclohexylamines / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D007211:Indoles / Q000737:chemistry; D020128:Inhibitory Concentration 50; D008562:Membrane Glycoproteins / Q000187:drug effects* / Q000378:metabolism; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects* / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D044263:Receptors, Serotonin, 5-HT1; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors / Q000378:metabolism / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000928:Antidepressive Agents; D002352:Carrier Proteins; D003514:Cyclohexylamines; D007211:Indoles; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D011942:Receptors, Adrenergic, alpha; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors; C493230:SLC6A4 protein, human; C493232:Slc6a4 protein, rat