Rizatriptan Benzoate

• CAT Number: A000349
• CAS Number: 145202-66-0
• Molecular Formula: C22H25N5O2
• Molecular Weight: 391.5
• Purity: ≥95%
• Target: 5-HT Receptor
• Solubility: Soluble in DMSO > 10 mM
• Storage: -20°C
• InChI: 1S/C15H19N5.C7H6O2/c1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20;8-7(9)6-4-2-1-3-5-6/h3-4,7-8,10-11,17H,5-6,9H2,1-2H3;1-5H,(H,8,9)
• InChIKey: JPRXYLQNJJVCMZ-UHFFFAOYSA-N
• SMILES: CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3.C1=CC=C(C=C1)C(=O)O

Rizatriptan Benzoate is a selective serotonin 5-HTID receptor agonist derived from tryptamine. Rizatriptan Benzoate is an activator of SR-1B. Rizatriptan benzoate selectively binds to and activates serotonin (5-HT) 1B receptors expressed in intracranial arteries, and to 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brain stem sensory nuclei. Receptor binding results in constriction of cranial vessels and inhibition of nociceptive transmission, thereby providing relief of migraine headaches..

Reference

1: Salehi S, Boddohi S. New formulation and approach for mucoadhesive buccal film
of rizatriptan benzoate. Prog Biomater. 2017 Nov 6. doi:
10.1007/s40204-017-0077-7. [Epub ahead of print] PubMed PMID: 29110144.

2: Girotra P, Singh SK. Multivariate Optimization of Rizatriptan Benzoate-Loaded
Solid Lipid Nanoparticles for Brain Targeting and Migraine Management. AAPS
PharmSciTech. 2017 Feb;18(2):517-528. doi: 10.1208/s12249-016-0532-0. Epub 2016
Apr 28. PubMed PMID: 27126007.

3: Madrakian T, Maleki S, Heidari M, Afkhami A. An electrochemical sensor for
rizatriptan benzoate determination using Fe3O4 nanoparticle/multiwall carbon
nanotube-modified glassy carbon electrode in real samples. Mater Sci Eng C Mater
Biol Appl. 2016 Jun;63:637-43. doi: 10.1016/j.msec.2016.03.041. Epub 2016 Mar 16.
PubMed PMID: 27040259.

4: Amolkumar K, Ashok T, Kiran J. Development and validation of UV
spectrophotometric method to study stress degradation behaviour of rizatriptan
benzoate. Guang Pu Xue Yu Guang Pu Fen Xi. 2015 Jan;35(1):137-40. PubMed PMID:
25993836.

5: Vidyadhara S, Sasidhar RL, Balakrishna T, Vardhan MS. Formulation of
rizatriptan benzoate fast dissolving buccal films by emulsion evaporation
technique. Int J Pharm Investig. 2015 Apr-Jun;5(2):101-6. doi:
10.4103/2230-973X.153387. PubMed PMID: 25838995; PubMed Central PMCID:
PMC4381386.

6: Bhagawati ST, Reddy MS, Avadani K, Muddukrishna BS, Dengale SJ, Bhat K.
Development and validation of reversed-phase high-performance liquid
chromatography method for estimation of rizatriptan benzoate in oral strip
formulations. J Basic Clin Pharm. 2014 Dec;6(1):7-11. doi:
10.4103/0976-0105.145766. PubMed PMID: 25538465; PubMed Central PMCID:
PMC4268631.

7: Bhagawati ST, Chonkar AD, Dengale SJ, Reddy SM, Bhat K. Bioavailability
Enhancement of Rizatriptan Benzoate by Oral Disintegrating Strip: In vitro and In
vivo Evaluation. Curr Drug Deliv. 2016;13(3):462-70. PubMed PMID: 26310617.

8: Avachat AM, Gujar KN, Wagh KV. Development and evaluation of tamarind seed
xyloglucan-based mucoadhesive buccal films of rizatriptan benzoate. Carbohydr
Polym. 2013 Jan 16;91(2):537-42. doi: 10.1016/j.carbpol.2012.08.062. Epub 2012
Sep 1. PubMed PMID: 23121942.

9: Yao G, Man Y, Luo X, Yu T, Ji L. Rizatriptan benzoate influences the
endogenous pain modulatory system in a rat model of migraine. Neural Regen Res.
2012 Jan 15;7(2):131-5. doi: 10.3969/j.issn.1673-5374.2012.02.009. PubMed PMID:
25767488; PubMed Central PMCID: PMC4354128.

10: Sundar BS, Suneetha A. Development and Validation of HPTLC Method for the
Estimation of Rizatriptan Benzoate in Bulk and Tablets. Indian J Pharm Sci. 2010
Nov;72(6):798-801. doi: 10.4103/0250-474X.84601. PubMed PMID: 21969758; PubMed
Central PMCID: PMC3178987.