Etoperidone

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Etoperidone
Clinical data
Trade namesSeveral
Other namesST-1191; McN-A-2673-11
Routes of
administration		By mouth
ATC code
Identifiers
  • 2-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-4,5-diethyl-1,2,4-triazol-3-one
JSmol)
  • Clc3cccc(N2CCN(CCCN1/N=C(\N(C1=O)CC)CC)CC2)c3
  • InChI=1S/C19H28ClN5O/c1-3-18-21-25(19(26)24(18)4-2)10-6-9-22-11-13-23(14-12-22)17-8-5-7-16(20)15-17/h5,7-8,15H,3-4,6,9-14H2,1-2H3 checkY
  • Key:IZBNNCFOBMGTQX-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Etoperidone, associated with several brand names, is an atypical antidepressant which was developed in the 1970s and either is no longer marketed or was never marketed.[1][2][3] It is a phenylpiperazine related to trazodone and nefazodone in chemical structure and is a serotonin antagonist and reuptake inhibitor (SARI) similarly to them.[4]

Medical uses

Etoperidone was used or was intended for use as an antidepressant in the treatment of depression.[1][5]

Pharmacology

Pharmacodynamics

Etoperidone[6]
Site Ki (nM) Species Ref
SERTTooltip Serotonin transporter 890 Human [7]
NETTooltip Norepinephrine transporter 20,000 Human [7]
DATTooltip Dopamine transporter 52,000 Human [7]
5-HT1A 85 Human [8]
5-HT2A 36 Human [8]
5-HT2C ? ? ?
α1 38 Human [8]
α2 570 Human [8]
D2
 2,300 Human [8]
H1 3,100 Human [8]
mAChTooltip Muscarinic acetylcholine receptor >35,000 Human [8][9]
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

Etoperidone is as an

monoamine transporters as well: serotonin transporter (890 nM) > norepinephrine transporter (20,000 nM) > dopamine transporter (52,000 nM).[7]

Pharmacokinetics

Etoperidone is

meta-chlorophenylpiperazine (mCPP), which likely accounts for its serotonergic effects.[10][11]

Chemistry

Etoperidone is a phenylpiperazine and is chemically related to nefazodone and trazodone.[3][12][13]

History

Etoperidone was discovered by scientists at

Micromedex's Index Nominum: International Drug Directory, etoperidone was indeed previously marketed in Spain and Italy.[1]

Society and culture

Generic names

Etoperidone is the

INNTooltip International Nonproprietary Name, while etoperidone hydrochloride is its USANTooltip United States Adopted Name.[15][1][5]

Brand names

Etoperidone has been associated with the brand names Axiomin, Centren, Depraser, Etonin, and Staff.[1][15][18]

Research

Etoperidone has been studied in dementia and found to be about as effective as thioridazine.[19]

See also

References

  1. ^
    ISBN 978-3-88763-075-1
    .
  2. ISBN 978-0-8155-1856-3
    .
  3. ^
    ISBN 978-3-527-66447-4
    .
  4. ISBN 978-0-323-37104-9
    .
  5. ^
    ISBN 978-94-011-4439-1
    .
  6. ^ Roth BL, Driscol J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.
  7. ^
    PMID 9537821
    .
  8. ^
    S2CID 21236268
    .
  9. PMID 8100134
    .
  10. S2CID 21305772
    .
  11. S2CID 24965789
    .
  12. ISBN 9783527645640
    .
  13. ISBN 9781461248286
    .
  14. PMID 3014372
    .
  15. ^
    ISBN 978-1-4757-2085-3
    .
  16. ^ "Proposed INN List 36" (PDF). Supplement to the WHO Chronicle. 30 (9). 1976.
  17. ^ "Recommended INN List 17" (PDF). Supplement to the WHO Chronicle. 31 (10). 1977.
  18. ^
    ISBN 978-0-8155-1856-3
    .
  19. PMID 11686961
    .

External links