Almotriptan

- CAS No.
- 154323-57-6
- Chemical Name:
- Almotriptan
- Synonyms
- LAS-31416;Almotriptan;LAS-31416-d6;ALMOTRIPTAN-D6;AlMotriptan API;Almotriptan, 10 mM in DMSO;ALMOTRIPTAN(SUBJECTTOPATENETFREE);1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulphonyl]pyrrolidine;N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-Indole-3-ethanamine;1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulphonyl]pyrrolidine-d6
- CBNumber:
- CB7716603
- Molecular Formula:
- C17H25N3O2S
- Molecular Weight:
- 335.46
- MOL File:
- 154323-57-6.mol
- Modify Date:
- 2025/1/27 9:38:02
Boiling point | 538.7±60.0 °C(Predicted) |
---|---|
Density | 1.27±0.1 g/cm3(Predicted) |
storage temp. | 2-8°C |
form | Solid |
pka | 16.92±0.30(Predicted) |
color | White to off-white |
CAS DataBase Reference | 154323-57-6(CAS DataBase Reference) |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H315-H319-H335 |
Precautionary statements | P233-P260-P261-P264-P270-P271-P280-P301+P312-P302+P352-P304-P304+P340-P305+P351+P338-P312-P321-P330-P332+P313-P337+P313-P340-P362-P403-P403+P233-P405-P501 |
Almotriptan Chemical Properties,Uses,Production
Description
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-HT1D/1B agonist with a 35 to 51-fold selectivity versus 5-HT1A 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-HT1B 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.
Uses
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 Preparation Products And Raw materials
Raw materials
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Venkatasai Life Sciences | +91-9908134868 +91-8008303069 | Hyderabad, India | 186 | 58 | Inquiry |
Rivashaa Agrotech Biopharma Pvt. Ltd. | +91-26463395 +91-7926462688 | Gujarat, India | 1615 | 58 | Inquiry |
SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6514 | 58 | Inquiry |
Pharma Affiliates | 172-5066494 | Haryana, India | 6754 | 58 | Inquiry |
CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6257 | 58 | Inquiry |
Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6739 | 58 | Inquiry |
Calidad Pharma Chemie | 08433672794 | Mumbai, India | 38 | 58 | Inquiry |
SMILAX LABORATORIES LIMITED | +91-40-23090260 | New Delhi, India | 6 | 58 | Inquiry |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 33024 | 60 | Inquiry |
career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29858 | 58 | Inquiry |
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