Almotriptan Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Almotriptan was first marketed in Spain as a new medicine against acute attacks of migraine. It is the fifth agent belonging to the “triptan” class to be launched after sumatriptan, naratriptan, zolmitriptan and rizatriptan. This close structural analog of sumatriptan can be prepared in six steps from 4-nitrobenzylsulfonyl chloride with a Fischer indole synthesis as the key step. Almotriptan acts as a dual 5-HT_1D/1B agonist with a 35 to 51-fold selectivity versus 5-HT_1A and 5-HT₇ receptors respectively as well as having insignificant affinity for the most relevant nonserotonergic receptors (K1＞1μM). Its agonistic effect on 5-HT,n receptors of trigeminal sensory neurons turns off neurogenic inflammation by inhibiting the release of neuropeptides such as calcitonin gene-related peptide, neurokinin A and substance P. Concomitantly, its action on the 5-HT_1B receptors in meningeal arteries relieves the vasodilatation of these vessels associated with migraine attacks. Almotriptan causes selective concentration-dependent vasoconstriction of human meningeal and temporal arteries (with EC₅₀ of 0.03 and 0.7 μM) compared to basilar (EC₅₀ = 3.5 μM) and pulmonary arteries (EC₅₀＞10μM) or rabbit mesenteric and renal arteries (EC₅₀＞100 μM). Although it is predominantly cleared by the kidneys as unchanged drug (45%) or transformed into inactive metabolites by monoamine oxidase A (MAO-A) and CYP3A4 enzymes in the liver, almotriptan has the highest oral bioavailability (70%) of the triptans and has a half-life of 3.5 h. The therapeutic dose of 12.5 mg is well tolerated, shows a rapid onset of action (30 min) and low recurrence rate compared to sumatriptan.

Verwenden

Serotonin 5HT1B /1D-receptor agonist

Definition

ChEBI: An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position.

Almotriptan Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Almotriptan Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32951	60
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29884	58
Xiamen AmoyChem Co., Ltd	+86-86-5926051114 +8618959220845	sales@amoychem.com	China	6383	58
Chongqing Chemdad Co., Ltd	+86-023-6139-8061 +86-86-13650506873	sales@chemdad.com	China	39894	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49374	58
SIMAGCHEM CORP	+86-13806087780	sale@simagchem.com	China	17365	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32080	58
AFINE CHEMICALS LIMITED	+86-0571-85134551	sales@afinechem.com	China	15354	58
Dayang Chem (Hangzhou) Co.,Ltd.	571-88938639 +8617705817739	info@dycnchem.com	China	52849	58
changzhou huayang technology co., ltd	+8615250961469	2571773637@qq.com	China	9725	58

154323-57-6()Verwandte Suche:

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• LAS-31416-d6
• ALMOTRIPTAN(SUBJECTTOPATENETFREE)
• Almotriptan
• N,N-Dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]-ethanamine
• dimethyl-[2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]ethyl]amine
• AlMotriptan API
• N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-Indole-3-ethanamine
• ALMOTRIPTAN-D6
• 1-[[[2-(Dimethyl-amino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine
• 1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulphonyl]pyrrolidine
• LAS-31416
• 1-[[[2-(Dimethyl-amino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine-d6
• 1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulphonyl]pyrrolidine-d6
• 1H-Indole-3-ethanamine, N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-
• AlmotriptanQ: What is Almotriptan Q: What is the CAS Number of Almotriptan Q: What is the storage condition of Almotriptan Q: What are the applications of Almotriptan
• 1-[[[3-[2- (Dimethylamino) ethyl]- 1H- indol-yl] sulfonyl] pyrrolidine - Base
• 154323-57-6
• C17H19D6N3O2S
• Intermediates & Fine Chemicals
• Isotope Labeled Compounds
• Pharmaceuticals
• APIs
• Isotope Labelled Compounds
• Heterocyclic Compounds