EXP-561 explained

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]}

Notes and References

1. US 3362878 - Pharmaceutical compositions and methods utilizing substituted bicyclo[2.2.2]-octanes
2. Fuller RW, Snoddy HD, Perry KW . Inhibition of amine uptake by 4-phenyl-bicyclo(2,2,2)octan-1-amine hydrochloride monohydrate (EXP 561) in rats . . 25 . 21 . 2409–10 . November 1976 . 999731 . 10.1016/0006-2952(76)90039-3.
3. Koe BK . 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 . December 1976 . 994022 . Koe BK .
4. Wong DT, Molloy BB, Bymaster FP . 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 . January 1977 . 834358 . 10.1016/0028-3908(77)90040-5. 44365500 .
5. Maj J, Skuza G, Sowińska H, Nowak G . Pharmacological properties of EXP 561, a potential antidepressant drug . Journal of Neural Transmission . 70 . 1–2 . 81–97 . 1987 . 2822850 . 10.1007/BF01252511. 23469131 .
6. US Patent 3308160 - PHENYLBICYCLO[Z.Z.Z]OCTANE-L-AMINES AND SALTS THEREOF
7. INTERNATIONAL REVIEW NEUROBIOLOGY, Volume 12 Page 160
8. Lehmann HE, Ban TA, Debow SL . A clinical-pharmacological study with EXP 561 . Current Therapeutic Research, Clinical and Experimental . 9 . 6 . 306–8 . June 1967 . 4963065 .
9. Gershon S, Hekimian LJ, Floyd A . 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 . February 1968 . 5695389 .
10. Ross SB, Kelder D . Inhibition of 3H-dopamine accumulation in reserpinized and normal rat striatum . Acta Pharmacologica et Toxicologica . 44 . 5 . 329–35 . May 1979 . 474143 . 10.1111/j.1600-0773.1979.tb02339.x.