Etoperidone

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Etoperidone
File:Etoperidone structure.svg
Systematic (IUPAC) name
2-[3-[4-(3-chlorophenyl)piperazin-1-yl]
propyl]-4,5-diethyl-1,2,4-triazol-3-one
Clinical data
Routes of
administration		 Oral
Legal status
Legal status
  • Uncontrolled
Identifiers
CAS Number 52942-31-1
ATC code N06AB09 (WHO)
PubChem CID 40589
Chemical data
Formula C19H28ClN5O
Molar mass 377.911 g/mol[[Script error: No such module "String".]]
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Etoperidone (Axiomin, Depracer, Etonin, Etoran, Staff, Tropene), also known as clopradone and thozalinone, is an antidepressant of the piperazine chemical class which was introduced in 1977, but has since been discontinued.

Etoperidone acts as an antagonist at a number of receptors in the following order of potency: 5-HT2 receptor (36 nM) > α1-adrenergic receptor (38 nM) > 5-HT1A receptor (85 nM) > α2-adrenergic receptor (570 nM).[1] It also has weak or negligible affinity for blocking the following receptors: D2 receptor (2,300 nM) > H1 receptor (3,100 nM) > muscarinic acetylcholine receptors (>35,000).[1] Etoperidone has weak affinity for the monoamine transporters as well: serotonin transporter (890 nM) > norepinephrine transporter (20,000) > dopamine transporter (52,000).[2]

Synthesis

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Palazzo, G.; 1974, U.S. Patent 3,857,845.

See also

References

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GABAA PAMs
Others
α2δ VDCC Blockers
5-HT1A Agonists
Azapirones: Buspirone • Gepirone • Tandospirone; Others: Flesinoxan • Oxaflozane
H1 Antagonists
Diphenylmethanes: Captodiame • Hydroxyzine; Others: Brompheniramine • Chlorpheniramine • Pheniramine
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
Others

M: PSO/PSI

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc, drug(N5A/5B/5C/6A/6B/6D)


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  1. ↑ 1.0 1.1 Cusack B, Nelson A, Richelson E. (19941). "Binding of Antidepressants to Human Brain Receptors: Focus on Newer Generation Compounds". Psychopharmacology (Berl). 114 (4): 559–565. doi:10.1007/BF02244985. PMID 7855217.  Check date values in: |date= (help)
  2. ↑ Tatsumi M, Groshan K, Blakely RD, Richelson E. (1997). "Pharmacological Profile of Antidepressants and Related Compounds at Human Monoamine Transporters". Eur J Pharmacol. 340 (2-3): 249–258. doi:10.1016/S0014-2999(97)01393-9. PMID 9537821. 
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