Etoperidone

Etoperidone

Etoperidone
Systematic (IUPAC) name
2-[3-[4-(3-chlorophenyl)piperazin-1-yl]
propyl]-4,5-diethyl-1,2,4-triazol-3-one
Clinical data
Legal status
  • (Prescription only)
Routes of
administration
Oral
Identifiers
CAS Registry Number  Y
ATC code N06
PubChem CID:
ChemSpider  Y
UNII  Y
ChEMBL  N
Synonyms ST-1191
Chemical data
Formula C19H28ClN5O
Molecular mass 377.911 g/mol
 N   

Etoperidone (Axiomin, Centren, Depracer, Etonin, Etoran, Staff, Tropene), also known as clopradone and triazolinone, is an antidepressant of the phenylpiperazine class which was introduced in Europe in 1977.[1][2] It acts primarily as an antagonist of several receptors in the following order of potency: 5-HT2A receptor (36 nM) > α1-adrenergic receptor (38 nM) > 5-HT1A receptor (85 nM) > α2-adrenergic receptor (570 nM);[3] it has only very weak or negligible affinity for blocking the following receptors: D2 receptor (2,300 nM) > H1 receptor (3,100 nM) > mACh receptors (>35,000 nM).[3] In addition to its receptor blockade, etoperidone also has weak affinity for the monoamine transporters as well: serotonin transporter (890 nM) > norepinephrine transporter (20,000 nM) > dopamine transporter (52,000 nM).[4]

See also

References

  1. ^ C. R Ganellin; D. J Triggle; F.. Macdonald (1997). Dictionary of pharmacological agents. CRC Press. p. 859.  
  2. ^ Index nominum 2000: international drug directory. Taylor & Francis US. 2000. p. 421.  
  3. ^ 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.  
  4. ^ 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.