181183-52-8
181183-52-8 structure
- Name: Almotriptan
- Chemical Name: almotriptan malate
- CAS Number: 181183-52-8
- Molecular Formula: C21H31N3O7S
- Molecular Weight: 469.552
- Catalog: Biochemical Inhibitor Neuronal Signaling 5-HT Receptor Agonist
- Create Date: 2018-09-07 13:47:33
- Modify Date: 2024-01-02 15:42:13
-
Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.IC50:Target: 5-hydroxytryptamine1B/1D (5-HT1B/1D) ReceptorAlmotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. Almotriptan showed low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors in several species, including the human, while affinity for 5-HT receptors other than 5-HT(1B/1D) was clearly less. Almotriptan did not exhibit significant affinity for several non-5-HT receptors studied up to 100 microM. Almotriptan inhibited forskolin-stimulated cyclic AMP accumulation in HeLa cells transfected with 5-HT(1B) or 5-HT(1D) human receptors [1]. Almotriptan had a mild antiemetic effect and a slight, transient diuretic effect in dogs, although the latter effect is probably of no clinical relevance. In addition, no effect on the respiratory system of conscious guinea pigs was observed following almotriptan treatment. These results indicate that almotriptan has a favourable safety profile with respect to the central nervous, renal and respiratory systems [2].
| Name | almotriptan malate |
|---|---|
| Synonyms |
2-Hydroxybutandisäure--N,N-dimethyl-2-{5-[(pyrrolidin-1-ylsulfonyl)methyl]-1H-indol-3-yl}ethanamin(1:1)
2-Hydroxysuccinic acid - N,N-dimethyl-2-{5-[(1-pyrrolidinylsulfonyl)methyl]-1H-indol-3-yl}ethanamine (1:1) N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]ethanamine,2-hydroxybutanedioic acid 2-hydroxybutanedioic acid - N,N-dimethyl-2-{5-[(pyrrolidin-1-ylsulfonyl)methyl]-1H-indol-3-yl}ethanamine (1:1) Almotriptan Malate N,N-Dimethyl-N-(2-(5-((1-pyrrolidinylsulfonyl)methyl)-1H-indol-2-yl)ethyl)amine - 2-Hydroxysuccinic Acid (1:1) 2-Hydroxysuccinic acid - N,N-dimethyl-2-{5-[(pyrrolidin-1-ylsulfonyl)methyl]-1H-indol-3-yl}ethanamine (1:1) ALMOTRIPTAN MALEATE Butanedioic acid, 2-hydroxy-, compd. with N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-indole-3-ethanamine (1:1) UNII:PJP312605E LAS 31416 dl-malate acid Axert butanedioic acid, 2-hydroxy-, compd. with 1-[[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine (1:1) acide 2-hydroxybutanedioïque - N,N-diméthyl-2-{5-[(pyrrolidin-1-ylsulfonyl)méthyl]-1H-indol-3-yl}éthanamine (1:1) 1-[[[3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine Hydroxybutanedioate (1:1) Almotriptan (malate) |
| Description | Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.IC50:Target: 5-hydroxytryptamine1B/1D (5-HT1B/1D) ReceptorAlmotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. Almotriptan showed low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors in several species, including the human, while affinity for 5-HT receptors other than 5-HT(1B/1D) was clearly less. Almotriptan did not exhibit significant affinity for several non-5-HT receptors studied up to 100 microM. Almotriptan inhibited forskolin-stimulated cyclic AMP accumulation in HeLa cells transfected with 5-HT(1B) or 5-HT(1D) human receptors [1]. Almotriptan had a mild antiemetic effect and a slight, transient diuretic effect in dogs, although the latter effect is probably of no clinical relevance. In addition, no effect on the respiratory system of conscious guinea pigs was observed following almotriptan treatment. These results indicate that almotriptan has a favourable safety profile with respect to the central nervous, renal and respiratory systems [2]. |
|---|---|
| Related Catalog | |
| References |
| Density | 1.27g/cm3 |
|---|---|
| Boiling Point | 538.7ºC at 760mmHg |
| Melting Point | 170-172ºC |
| Molecular Formula | C21H31N3O7S |
| Molecular Weight | 469.552 |
| Flash Point | 279.6ºC |
| Exact Mass | 469.188263 |
| PSA | 159.62000 |
| LogP | 2.12290 |
| Vapour Pressure | 1.13E-11mmHg at 25°C |
| Storage condition | -20°C Freezer |
| RIDADR | NONH for all modes of transport |
|---|
|
~99%
181183-52-8 |
| Literature: MSN LABORATORIES LIMITED; SATYANARAYANA REDDY, Manne; ESWARAIAH, Sajja; SAHADEVA REDDY, Maramreddy; SATYANARAYANA, Komati Patent: WO2010/113183 A2, 2010 ; Location in patent: Page/Page column 26 ; |
|
~%
181183-52-8 |
| Literature: US2008/234495 A1, ; Page/Page column 3 ; |
|
~%
181183-52-8 |
| Literature: US2008/234495 A1, ; Page/Page column 3 ; |
| Precursor 2 | |
|---|---|
| DownStream 0 | |