|
| Product Name: | Rizatriptan benzoate | | Synonyms: | RIZATRIPTAN BENZOATE;N,N-DIMETHYL-5-(1H-1,2,4-TRIAZOL-1-YLMETHYL)-1H-INDOLE-3-ETHANAMINE, BENZOATE;n,n-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1h-indol-3-yl]ethylamine benzoate;Rizatrimptan Benzoate;Rizatrimptan;Rizatriptan monobenzoate;N,N-Dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-;Acid Bixente triptans | | CAS: | 145202-66-0 | | MF: | C22H25N5O2 | | MW: | 391.48 | | EINECS: | 604-465-6 | | Product Categories: | MK-462, Maxalt;Heterocycles;API;Intermediates & Fine Chemicals;Neurochemicals;Pharmaceuticals;Antimigraine;Heterocyclic Compounds;Rizatriptan;Amines | | Mol File: | 145202-66-0.mol |  |
| | Rizatriptan benzoate Chemical Properties |
| Melting point | 178-180°C | | storage temp. | 2-8°C | | solubility | H2O: ≥5mg/mL | | form | powder | | color | white to beige | | Merck | 14,8241 | | InChIKey | JPRXYLQNJJVCMZ-UHFFFAOYSA-N | | CAS DataBase Reference | 145202-66-0(CAS DataBase Reference) |
| Hazard Codes | T | | Risk Statements | 61 | | WGK Germany | 3 | | HS Code | 2933995500 |
| | Rizatriptan benzoate Usage And Synthesis |
| Description | Known as a 5-hydroxytryptamine agonist, Rizatriptan Benzoate is the benzoate salt form of rizatriptan with anti-migraine activity, which can be used to treat the migraine headaches. It is FDA-approved to use in the treatment of acute migraine attacks with or without aura, especially taken at the first sign of a migraine headache. However, it cannot prevent future migraine attacks and it is ineffective to prevent other types of headache.
The pain of migraine headaches is believed to be induced by dilated blood vessels inside the head. Rizatriptan Benzoate relieves the pain by inducing vasoconstriction, which functions as an agonist at serotonin 5-HT1B and 5-HT1D receptors. The selective receptor binding is effective to constrict cranial vessels and inhibit the transmission of nociception, thus providing relief of migraine headaches.
| | References | https://en.wikipedia.org/wiki/Rizatriptan
https://pubchem.ncbi.nlm.nih.gov/compound/77997#section=Top
http://bodyandhealth.canada.com/drug/getdrug/co-rizatriptan-odt
| | Description | Rizatriptan was launched for the first time as Maxalt in Mexico for the
acute treatment of migraine headaches with or without aura in adults. It is the
third in a new generation of triptan migraine drugs to challenge the firstgeneration
product Sumatriptan from Glaxo Wellcome, after Zolmitriptan
(Zeneca) and Naratriptan (Glaxo Wellcome).
It can be synthetically obtained by two related routes having respectively 3 and 4
steps, both starting from 1 -(4-aminobenzyl)-l,2,4-triazole. Rizatriptan is a full 5-HT1D/1B receptor agonist retaining a significant affinity at 5-HT1A sites (pIC50
= 6.4), with a low affinity for nond-HT sites. It shows craniovascufar selectivity
for human isolated middle meningeal over coronary arteries ; its effect on
coronary artery constriction is significantly less than that for Sumatriptan.
Rizatriptan inhibits the release of neuropeptides that cause swelling of cranial
blood vessels. Rizatriptan has a good oral bioavailability (64% and 47% in rats
and dogs respectively). and a rapid onset of action : the headache relief in
human occurs within 30 to 45 minutes of taking 20 mg. It also relieved nausea
and hypersensitivity to noise (phonophobia) and light (photophobia) that are
often symptoms accompanying a migraine attack. Among at least 6 metabolites
identified in humans after a single oral dose (60 mg), the major urinary
metabolite was the corresponding indole-3-acetic acid. Maxalt is available as a
novel oral formulation of rapidly dissolving tablets or wafers that does not require
liquid for ingestion. | | Chemical Properties | Off-White Solid | | Originator | Merck & Co (US) | | Uses | Rizatriptan Benzoate(Maxalt) is a 5-HT1 agonist triptan drug for the treatment of migraine headaches. It is believed to work by narrowing the blood vessels around the brain. Rizatriptan also reduces the substances in the body, which can also reduce headac | | Uses | A selective serotonin 5-HTID receptor agonist. Structurally derived from tryptamine | | Uses | Rizatriptan Benzoate is a selective serotonin 5-HTID receptor agonist and used to treat migraine (1,2,3). It is structurally derived from tryptamine. | | Definition | ChEBI: Rizatriptan benzoate is a member of tryptamines. | | Brand name | Maxalt (Merck). | | General Description | Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards | | Biochem/physiol Actions | Rizatriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine. |
| | Rizatriptan benzoate Preparation Products And Raw materials |
|
