Английская Википедия:Amesergide
Шаблон:Short description Шаблон:Drugbox
Amesergide (Шаблон:Abbrlink, Шаблон:Abbrlink; developmental code name LY-237733) is a serotonin receptor antagonist of the ergoline and lysergamide families related to methysergide which was under development by Eli Lilly and Company for the treatment of a variety of conditions including depression, anxiety, schizophrenia, male sexual dysfunction, migraine, and thrombosis but was never marketed.[1][2][3] It reached phase II clinical trials for the treatment of depression, erectile dysfunction, and premature ejaculation prior to the discontinuation of its development.[1]
Pharmacology
Pharmacodynamics
Amesergide acts as a selective antagonist of the serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptors (Ki = 1.96–15.1 nM).[4][5] It is also an antagonist of the serotonin 5-HT7 receptor with relatively lower affinity (Ki = 78.0 nM).[6] The drug is a potent antagonist of the α2-adrenergic receptor in addition to the 5-HT2 receptors via its major active metabolite 4-hydroxyamesergide (Ki = 13 nM).[7][8] This profile of activity is similar to that of the so-called noradrenergic and specific serotonergic antidepressant (NaSSA) mirtazapine (Remeron).[9]
Amesergide also has affinity for the serotonin 5-HT1D receptor (Ki = 57.9 nM) and lower affinity for the serotonin 5-HT1A, α1-adrenergic, and dopamine D1 and D2 receptors (Ki = 150–730 nM).[4] It has negligible affinity for the histamine H1 and muscarinic acetylcholine receptors (Ki > 10,000 nM).[4] The drug does not appear to have been assessed at the serotonin 5-HT1E, 5-HT1F, 5-HT4, 5-HT5A, and 5-HT6 receptors, nor at the dopamine D3, D4, and D5 receptors.[10]
| Site | Affinity (Ki [nM]) | Species | Source |
|---|---|---|---|
| 5-HT1A | 177.3 | Rat | [4] |
| 5-HT1B | ? | ? | ? |
| 5-HT1D | 57.9 | Cow | [4] |
| 5-HT2A | 15.1 12.4 |
Human Rat |
[5] [4] |
| 5-HT2B | 1.96 | Human | [5] |
| 5-HT2C | 6.27 13.27 |
Human Pig |
[5] [4] |
| 5-HT3 | >10,000 | Rat | [4] |
| 5-HT6 | ? | ? | ? |
| 5-HT7 | 78.0 | Human | [11] |
| α1 | 730 | Rat | [4] |
| α2 | 50 13 (Шаблон:Abbr) |
Rat | [4] [7] |
| β | >10,000 | Rat | [4] |
| D1 | 150 | Rat | [4] |
| D2 | 520 | Rat | [4] |
| H1 | >10,000 | Rat | [4] |
| Шаблон:Abbrlink | >10,000 | Rat | [4] |
| Notes: The smaller the affinity value, the more strongly the drug binds to the site. | |||
References
External links
Шаблон:Navboxes Шаблон:Ergolines
- ↑ 1,0 1,1 Шаблон:Cite web
- ↑ Шаблон:Cite book
- ↑ Шаблон:Cite book
- ↑ 4,00 4,01 4,02 4,03 4,04 4,05 4,06 4,07 4,08 4,09 4,10 4,11 4,12 4,13 4,14 Шаблон:Cite journal
- ↑ 5,0 5,1 5,2 5,3 Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ 7,0 7,1 Шаблон:Cite journal
- ↑ Шаблон:Cite book
- ↑ Шаблон:Cite journal
- ↑ 10,0 10,1 Шаблон:Cite web
- ↑ Шаблон:Cite journal
- Английская Википедия
- 5-HT2A antagonists
- 5-HT2B antagonists
- 5-HT2C antagonists
- 5-HT7 antagonists
- Abandoned drugs
- Alpha-2 blockers
- Antidepressants
- Anxiolytics
- Isopropyl compounds
- Lysergamides
- Страницы, где используется шаблон "Навигационная таблица/Телепорт"
- Страницы с телепортом
- Википедия
- Статья из Википедии
- Статья из Английской Википедии
