CAS 181183-52-8|Almotriptan

Introduction：Basic information about CAS 181183-52-8|Almotriptan, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Almotriptan BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

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	ChineseUSA	Flash Point	279.6ºC

Names

Name	almotriptan malate
Synonym	More Synonyms

Almotriptan BiologicalActivity

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	Research Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor
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.

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

Research Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor

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
InChIKey	QHATUKWEVNMHRY-UHFFFAOYSA-N
SMILES	CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N3CCCC3)cc12.O=C(O)CC(O)C(=O)O
Storage condition	-20°C Freezer

Safety Information

RIDADR	NONH for all modes of transport

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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