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Etoperidone
Systematic (IUPAC) name
2-[3-[4-(3-chlorophenyl)piperazin-1-yl]
propyl]-4,5-diethyl-1,2,4-triazol-3-one
Identifiers
CAS number 52942-31-1
ATC code N06AB09
PubChem 40589
Chemical data
Formula C 19H28ClN5O 
Mol. mass 377.911 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status Uncontrolled
Routes Oral

Etoperidone (Axiomin, Depracer, Etonin, Etoran, Staff, Tropene), also known as clopradone and thozalinone, is an antidepressant drug of the piperazine chemical class which was introduced in 1977, but has subsequently been discontinued. It is closely related to trazodone and nefazodone both structurally and pharmacologically.

Pharmacology

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]

References

  1. ^ a b 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. PMID 7855217.  
  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. PMID 9537821.  







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