Rizatriptan benzoate

Names

[ Name ]:
Rizatriptan benzoate

[Synonym ]:
Rizatriptan benzoate salt
N,N-Dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indole-3-ethanamine monobenzoate
N,N-dimethyl-2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine benzoate
Rizatriptan benzoate
1H-Indole-3-ethanamine, N,N-dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-, benzoate (1:1)
N,N-Dimethyl-2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine benzoate (1:1)
Maxalt
MK-462 (N,N-Dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine benzoate salt
Rizatrimptan benzoate
MFCD00866224
Benzolcarbonsäure--N,N-dimethyl-2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamin(1:1)
N,N-diméthyl-2-[5-(1H-1,2,4-triazol-1-ylméthyl)-1H-indol-3-yl]éthanamine benzoate
Rizatriptan
N,N-Dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine Benzoate

Biological Activity

[Description]:

Rizatriptan Benzoate(Maxalt) is a 5-HT1 agonist triptan drug for the treatment of migraine headaches.Target: 5-HT1 agonist 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 headache pain, nausea, sensitivity to light and sound and other migraine symptoms.Rizatriptan was rapidly absorbed with a median tmax of 1.3 h (range 1-3 h) vs a tmax for sumatriptan of 2.5 h (range 1-4 h, P < 0.001). Administration of either rizatriptan or sumatriptan produced maximal mean elevations of 5-10 mmHg in systolic and diastolic blood pressures without effect on heart rate; the changes occurred sooner following rizatriptan, consistent with more rapid absorption. Both rizatriptan and sumatriptan provoked mild increases in serum growth hormone without any effect on serum prolactin concentrations. The most commonly reported symptom following rizatriptan was drowsiness.

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[References]

[1]. Sciberras DG, et al. Initial human experience with MK-462 (rizatriptan): a novel 5-HT1D agonist. Br J Clin Pharmacol. 1997 Jan;43(1):49-54.

Chemical & Physical Properties

[ Density]:
1.21g/cm3

[ Boiling Point ]:
504.8ºC at 760mmHg

[ Melting Point ]:
178-180°C

[ Molecular Formula ]:
C₂₂H₂₅N₅O₂

[ Molecular Weight ]:
391.466

[ Flash Point ]:
259.1ºC

[ Exact Mass ]:
391.200836

[ PSA ]:
87.04000

[ LogP ]:
3.29660

[ Vapour Pressure ]:
2.58E-10mmHg at 25°C

[ Index of Refraction ]:
1.645

[ Storage condition ]:
-20°C Freezer

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS08

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H360

[ Precautionary Statements ]:
P201-P280-P308 + P313

[ Hazard Codes ]:
C,Xi

[ Risk Phrases ]:
R34:Causes burns.

[ Safety Phrases ]:
S26-S36/37/39-S45

[ RIDADR ]:
3259

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

Evolution of paediatric off-label use after new significant medicines become available for adults: a study on triptans in Finnish children 1994-2007.

Br. J. Clin. Pharmacol. 71(6) , 929-35, (2011)

• Off-label use in children is widespread. New medicines lack marketing authorization for paediatric use, even when they represent significant therapeutic advantages and are intended for treatment of ...

An approach for rapid development of nasal delivery of analgesics--identification of relevant features, in vitro screening and in vivo verification.

Int. J. Pharm. 420(1) , 43-50, (2011)

Drug delivery via the nasal route is gaining increasing interest over the last two decades as an alternative to oral or parenteral drug administration. In the current study an approach for rapid ident...

Efficacy and tolerability of rizatriptan for the treatment of acute migraine in sumatriptan non-responders.

Cephalalgia 31(7) , 786-96, (2011)

The study was carried out to assess the efficacy and tolerability of rizatriptan orally disintegrating tablet (ODT) for treating acute migraine in patients who are non-responders to sumatriptan.Many m...