From Wikipedia, the free encyclopedia
Chemical compound
EXP-561
[1] is an
investigational drug that acts as an
inhibitor of the
reuptake of
serotonin ,
dopamine , and
norepinephrine .
[2]
[3]
[4]
[5] It was developed in the 1960s by Du Pont
[6] and was suggested as a potential
antidepressant but failed in trials
[7] and was never marketed.
[5]
[8]
[9]
[10]
References
^ US 3362878 - Pharmaceutical compositions and methods utilizing substituted bicyclo[2.2.2]-octanes
^ Fuller RW, Snoddy HD, Perry KW (November 1976). "Inhibition of amine uptake by 4-phenyl-bicyclo(2,2,2)octan-1-amine hydrochloride monohydrate (EXP 561) in rats".
Biochemical Pharmacology . 25 (21): 2409–10.
doi :
10.1016/0006-2952(76)90039-3 .
PMID
999731 .
^
Koe BK (December 1976).
"Molecular geometry of inhibitors of the uptake of catecholamines and serotonin in synaptosomal preparations of rat brain" . The Journal of Pharmacology and Experimental Therapeutics . 199 (3): 649–61.
PMID
994022 .
^ Wong DT, Molloy BB, Bymaster FP (January 1977). "Blockade of monoamine uptake by 1-amino-4-phenylbicyclo(2,2,2)octane (EXP 561) in rat brain and heart". Neuropharmacology . 16 (1): 11–5.
doi :
10.1016/0028-3908(77)90040-5 .
PMID
834358 .
S2CID
44365500 .
^
a
b Maj J, Skuza G, Sowińska H, Nowak G (1987). "Pharmacological properties of EXP 561, a potential antidepressant drug". Journal of Neural Transmission . 70 (1–2): 81–97.
doi :
10.1007/BF01252511 .
PMID
2822850 .
S2CID
23469131 .
^ US Patent 3308160 - PHENYLBICYCLO[Z.Z.Z]OCTANE-L-AMINES AND SALTS THEREOF
^ INTERNATIONAL REVIEW NEUROBIOLOGY, Volume 12 Page 160
^ Lehmann HE, Ban TA, Debow SL (June 1967). "A clinical-pharmacological study with EXP 561". Current Therapeutic Research, Clinical and Experimental . 9 (6): 306–8.
PMID
4963065 .
^ Gershon S, Hekimian LJ, Floyd A (February 1968). "Non-correlation of preclinical-clinical evaluation of a prosposed anti-depressant 4-phenyl-bicyclo(2,2,2)octan-1-amine hydrochloride monohydrate (EXP 561)". Arzneimittel-Forschung . 18 (2): 243–5.
PMID
5695389 .
^ Ross SB, Kelder D (May 1979). "Inhibition of 3H-dopamine accumulation in reserpinized and normal rat striatum". Acta Pharmacologica et Toxicologica . 44 (5): 329–35.
doi :
10.1111/j.1600-0773.1979.tb02339.x .
PMID
474143 .
SSRIs Tooltip Selective serotonin reuptake inhibitors
SNRIs Tooltip Serotonin–norepinephrine reuptake inhibitors
NRIs Tooltip Norepinephrine reuptake inhibitors
NDRIs Tooltip Norepinephrine–dopamine reuptake inhibitors
NaSSAs Tooltip Noradrenergic and specific serotonergic antidepressants
SARIs Tooltip Serotonin antagonist and reuptake inhibitors
SMS Tooltip Serotonin modulator and stimulators Others
TCAs Tooltip Tricyclic antidepressants
TeCAs Tooltip Tetracyclic antidepressants Others
Non-selective
MAOA Tooltip Monoamine oxidase A -selective
MAOB Tooltip Monoamine oxidase B -selective
DAT Tooltip Dopamine transporter (
DRIs Tooltip Dopamine reuptake inhibitors )
NET Tooltip Norepinephrine transporter (
NRIs Tooltip Norepinephrine reuptake inhibitors )
Others:
Antihistamines (e.g.,
brompheniramine ,
chlorphenamine ,
pheniramine ,
tripelennamine )
Antipsychotics (e.g.,
loxapine ,
ziprasidone )
Arylcyclohexylamines (e.g.,
ketamine ,
phencyclidine )
Dopexamine
Ephenidine
Ginkgo biloba
Indeloxazine
Nefazodone
Opioids (e.g.,
desmetramadol ,
methadone ,
pethidine (meperidine) ,
tapentadol ,
tramadol ,
levorphanol )
SERT Tooltip Serotonin transporter (
SRIs Tooltip Serotonin reuptake inhibitors )
Others:
A-80426
Amoxapine
Antihistamines (e.g.,
brompheniramine ,
chlorphenamine ,
dimenhydrinate ,
diphenhydramine ,
mepyramine (pyrilamine) ,
pheniramine ,
tripelennamine )
Antipsychotics (e.g.,
loxapine ,
ziprasidone )
Arylcyclohexylamines (e.g.,
3-MeO-PCP ,
esketamine ,
ketamine ,
methoxetamine ,
phencyclidine )
Cyclobenzaprine
Delucemine
Dextromethorphan
Dextrorphan
Efavirenz
Hypidone
Medifoxamine
Mesembrine
Mifepristone
MIN-117 (WF-516)
N-Me-5-HT
Opioids (e.g.,
dextropropoxyphene ,
methadone ,
pethidine (meperidine) ,
levorphanol ,
tapentadol ,
tramadol )
Roxindole
VMATs Tooltip Vesicular monoamine transporters Others