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
Pregnancy cat.	?
Legal status	℞ Prescription only
Routes	Oral
Identifiers
CAS number	52942-31-1
ATC code	N06AB09
PubChem	CID 40589
ChemSpider	37083
UNII	KAI6MVO39Z
Synonyms	ST-1191
Chemical data
Formula	C19H28ClN5O
Mol. mass	377.911 g/mol
SMILES	eMolecules & PubChem
	InChI 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 ; Key:IZBNNCFOBMGTQX-UHFFFAOYSA-N ;
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Etoperidone (Axiomin, Centren, Depracer, Etonin, Etoran, Staff, Tropene), also known as clopradone and thozalinone, 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-HT_2A receptor (36 nM) > α₁-adrenergic receptor (38 nM) > 5-HT_1A 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]

[edit] See also

^ C. R Ganellin; D. J Triggle; F.. Macdonald (1997). Dictionary of pharmacological agents. CRC Press. p. 859. ISBN 978-0-412-46630-4. http://books.google.com/books?id=DeX7jgInYFMC&pg=PA859. Retrieved 27 November 2011.
^ Index nominum 2000: international drug directory. Taylor & Francis US. 2000. p. 421. ISBN 978-3-88763-075-1. http://books.google.com/books?id=5GpcTQD_L2oC&pg=PA421. Retrieved 27 November 2011.
^ ^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. doi:10.1007/BF02244985. PMID 7855217.
^ 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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Systematic (IUPAC) name
2-[3-[4-(3-chlorophenyl)piperazin-1-yl] propyl]-4,5-diethyl-1,2,4-triazol-3-one
Clinical data
Pregnancy cat.	?
Legal status	℞ Prescription only
Routes	Oral
Identifiers
CAS number	52942-31-1
ATC code	N06AB09
PubChem	CID 40589
ChemSpider	37083^Y
UNII	KAI6MVO39Z^Y
Synonyms	ST-1191
Chemical data
Formula	C₁₉H₂₈Cl N₅O
Mol. mass	377.911 g/mol
SMILES	eMolecules & PubChem
InChI 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^Y Key:IZBNNCFOBMGTQX-UHFFFAOYSA-N^Y
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