Английская Википедия:Etoperidone
Шаблон:Short description Шаблон:Drugbox
Etoperidone, associated with several brand names, is an atypical antidepressant which was developed in the 1970s and either is no longer marketed or was never marketed.[1][2][3] It is a phenylpiperazine related to trazodone and nefazodone in chemical structure and is a serotonin antagonist and reuptake inhibitor (SARI) similarly to them.[4]
Medical uses
Etoperidone was used or was intended for use as an antidepressant in the treatment of depression.[1][5]
Pharmacology
Pharmacodynamics
Site | Ki (nM) | Species | Ref |
---|---|---|---|
Шаблон:Abbrlink | 890 | Human | [7] |
Шаблон:Abbrlink | 20,000 | Human | [7] |
Шаблон:Abbrlink | 52,000 | Human | [7] |
5-HT1A | 85 | Human | [8] |
5-HT2A | 36 | Human | [8] |
5-HT2C | ? | ? | ? |
α1 | 38 | Human | [8] |
α2 | 570 | Human | [8] |
D2 | 2,300 | Human | [8] |
H1 | 3,100 | Human | [8] |
Шаблон:Abbrlink | >35,000 | Human | [8][9] |
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. |
Etoperidone is 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) (may be a partial agonist) > α2-adrenergic receptor (570 nM);[8] 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).[8] 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).[7]
Pharmacokinetics
Etoperidone is metabolized in part to meta-chlorophenylpiperazine (mCPP), which likely accounts for its serotonergic effects.[10][11]
Chemistry
Etoperidone is a phenylpiperazine and is chemically related to nefazodone and trazodone.[3][12][13]
History
Etoperidone was discovered by scientists at Angelini, who also discovered trazodone.[14] Its development names have included ST-1191 and McN-A-2673-11.[15][1] The Шаблон:Abbrlink etoperidone was proposed in 1976 and recommended in 1977.[16][17] The drug was given brand names in Spain (Centren (Esteve) and Depraser (Lepori)) and Italy (Staff (Sigma Tau))[1] and was also given the brand names Axiomin and Etonin,[15] but it is not entirely clear if it was actually marketed; the Pharmaceutical Manufacturing Encyclopedia provides no dates for commercial introduction.[18] According to Micromedex's Index Nominum: International Drug Directory, etoperidone was indeed previously marketed in Spain and Italy.[1]
Society and culture
Generic names
Etoperidone is the generic name of the drug and its Шаблон:Abbrlink, while etoperidone hydrochloride is its Шаблон:Abbrlink.[15][1][5]
Brand names
Etoperidone has been associated with the brand names Axiomin, Centren, Depraser, Etonin, and Staff.[1][15][18]
Research
Etoperidone has been studied in dementia and found to be about as effective as thioridazine.[19]
See also
References
External links
Шаблон:Antidepressants Шаблон:Anxiolytics Шаблон:Navboxes
- ↑ 1,0 1,1 1,2 1,3 1,4 1,5 1,6 Шаблон:Cite book
- ↑ Шаблон:Cite book
- ↑ 3,0 3,1 Шаблон:Cite book
- ↑ Шаблон:Cite book
- ↑ 5,0 5,1 Шаблон:Cite book
- ↑ Шаблон:Cite web
- ↑ 7,0 7,1 7,2 7,3 Шаблон:Cite journal
- ↑ 8,0 8,1 8,2 8,3 8,4 8,5 8,6 8,7 8,8 Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite book
- ↑ Шаблон:Cite book
- ↑ Шаблон:Cite journal
- ↑ 15,0 15,1 15,2 15,3 Шаблон:Cite book
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ 18,0 18,1 Шаблон:Cite book
- ↑ Шаблон:Cite journal
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