Etoperidon

Etoperidon
(IUPAC) ime
	2-[3-[4-(3-hlorofenil)piperazin-1-il]; propil]-4,5-dietil-1,2,4-triazol-3-on
Klinički podaci
Identifikatori
CAS broj	52942-31-1
ATC kod	N06AB09
PubChem	40589
ChemSpider	37083
UNII	KAI6MVO39Z
Hemijski podaci
Formula	C19H28ClN5O
Mol. masa	377,911 g/mol
SMILES	eMolekuli & PubHem
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
Sinonimi	ST-1191
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	℞ Prescription only
Način primene	Oralno

Etoperidon (Aksiomin, Centren, Depracer, Etonin, Etoran, Staf, Tropen, klopradon, tozalinon) je antidepresiv iz fenilpiperazinske klase koji je uveden u upotrebu u Evropi 1977.^[4]^[5] On prvenstveno deluje kao antagonist nekoliko receptora u sledećem redosledu potencije: 5-HT_2A receptor (36 nM) > α₁-adrenergički receptor (38 nM) > 5-HT_1A receptor (85 nM) > α₂-adrenergički receptor (570 nM);^[6] on ima zanemarljiv afinitet za blokiranje sledećih receptora: D₂ receptor (2.300 nM) > H₁ receptor (3,100 nM) > mACh receptori (>35.000 nM).^[6] Pored blokiranja receptora, etoperidon isto tako ima slab afinitet za monoaminske transportere kao i za: serotoninski transporter (890 nM) > norepinefrinski transporter (20.000 nM) > dopaminski transporter (52.000 nM).^[7]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ C. R Ganellin; D. J Triggle; F.. Macdonald (1997). Dictionary of pharmacological agents. CRC Press. str. 859. ISBN 978-0-412-46630-4. Pristupljeno 27 November 2011.
↑ Index nominum 2000: international drug directory. Taylor & Francis US. 2000. str. 421. ISBN 978-3-88763-075-1. Pristupljeno 27 November 2011.
↑ ^6,0 ^6,1 Cusack B, Nelson A, Richelson E. (1994). „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.

Literatura

Index nominum 2000: international drug directory. Taylor & Francis US. 2000. str. 421. ISBN 978-3-88763-075-1. Pristupljeno 27 November 2011.
C. R Ganellin; D. J Triggle; F.. Macdonald (1997). Dictionary of pharmacological agents. CRC Press. str. 859. ISBN 978-0-412-46630-4. Pristupljeno 27 November 2011.

Povezano

Serotoninski antagonist i inhibitor preuzimanja

Vanjske veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[GanellinTriggle1997-4] C. R Ganellin; D. J Triggle; F.. Macdonald (1997). Dictionary of pharmacological agents. CRC Press. str. 859. ISBN 978-0-412-46630-4. Pristupljeno 27 November 2011.

[Index_nominum_2000:_international_drug_directory-5] Index nominum 2000: international drug directory. Taylor & Francis US. 2000. str. 421. ISBN 978-3-88763-075-1. Pristupljeno 27 November 2011.

[pmid7855217-6] 6,0 ^6,1 Cusack B, Nelson A, Richelson E. (1994). „Binding of Antidepressants to Human Brain Receptors: Focus on Newer Generation Compounds.”. Psychopharmacology (Berl). 114 (4): 559–565. DOI:10.1007/BF02244985. PMID 7855217.

[pmid9537821-7] 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.

[4]