Chemistry:EXP-561

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Short description: Chemical compound
EXP-561
EXP-561.svg
Clinical data
Routes of
administration
Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC14H19N
Molar mass201.313 g·mol−1
3D model (JSmol)

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

  1. US 3362878 - Pharmaceutical compositions and methods utilizing substituted bicyclo[2.2.2]-octanes
  2. "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. November 1976. doi:10.1016/0006-2952(76)90039-3. PMID 999731. 
  3. 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. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=994022. 
  4. "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. doi:10.1016/0028-3908(77)90040-5. PMID 834358. 
  5. 5.0 5.1 "Pharmacological properties of EXP 561, a potential antidepressant drug". Journal of Neural Transmission 70 (1–2): 81–97. 1987. doi:10.1007/BF01252511. PMID 2822850. 
  6. US Patent 3308160 - PHENYLBICYCLO[Z.Z.Z]OCTANE-L-AMINES AND SALTS THEREOF
  7. INTERNATIONAL REVIEW NEUROBIOLOGY, Volume 12 Page 160
  8. "A clinical-pharmacological study with EXP 561". Current Therapeutic Research, Clinical and Experimental 9 (6): 306–8. June 1967. PMID 4963065. 
  9. "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. PMID 5695389. 
  10. "Inhibition of 3H-dopamine accumulation in reserpinized and normal rat striatum". Acta Pharmacologica et Toxicologica 44 (5): 329–35. May 1979. doi:10.1111/j.1600-0773.1979.tb02339.x. PMID 474143.