Almotriptan

Modify Date: 2024-01-02 15:42:13

Almotriptan Structure
Almotriptan structure
Common Name Almotriptan
CAS Number 181183-52-8 Molecular Weight 469.552
Density 1.27g/cm3 Boiling Point 538.7ºC at 760mmHg
Molecular Formula C21H31N3O7S Melting Point 170-172ºC
MSDS Chinese USA Flash Point 279.6ºC

 Use of Almotriptan


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].

 Names

Name almotriptan malate
Synonym More Synonyms

 Almotriptan Biological Activity

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

[1]. Bou J , et al. Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine. Eur J Pharmacol, 2000. 410(1): p. 33-41.

[2]. Gras J, et al. Safety profile of almotriptan, a new antimigraine agent. Effects on central nervous system, renal function and respiratory dynamics. Arzneimittelforschung, 2001. 51(9): p. 726-32.

 Chemical & Physical Properties

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

 Safety Information

RIDADR NONH for all modes of transport

 Synthetic Route

~99%

Almotriptan Structure

Almotriptan

CAS#: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 ;

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Almotriptan Structure

Almotriptan

CAS#:181183-52-8

Literature: US2008/234495 A1, ; Page/Page column 3 ;

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Almotriptan Structure

Almotriptan

CAS#:181183-52-8

Literature: US2008/234495 A1, ; Page/Page column 3 ;

 Precursor & DownStream

Precursor  2

DownStream  0

 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)
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