[CAS NO. 145202-66-0] Rizatriptanbenzoate

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PRODUCTS SPECIFICATIONS [145202-66-0]

Catalog

HY-B0206

Brand

MCE

CAS

145202-66-0

DESCRIPTION [145202-66-0]

Overview

MDL	MFCD00866224
Molecular Weight	391.47
Molecular Formula	C22H25N5O2
SMILES	CN(C)CCC1=CNC2=C1C=C(CN3N=CN=C3)C=C2.O=C(O)C4=CC=CC=C4

For research use only. We do not sell to patients.

Summary

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.

IC50 & Target

5-HT ₁ Receptor

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00095004	Organon and Co	Migraine	October 21, 2004	Phase 3
NCT00898677	Organon and Co	Migraine Headache	September 1995	Phase 3
NCT00516737	Organon and Co	Migraine	October 3, 2007	Phase 3
NCT01004263	Organon and Co	Acute Migraine With or Without Aura in Adolescents	December 1, 2009	Phase 3
NCT00111709	Organon and Co	Migraine	May 27, 2005	Phase 3
NCT00111722	Organon and Co	Migraine	May 27, 2005	Phase 3
NCT00092963	Organon and Co	Migraine	August 17, 2004	Phase 3
NCT00812006	Organon and Co	Migraine	March 24, 2009	Phase 3
NCT00604812	Organon and Co	Migraine Disorders	December 17, 2007	Phase 1
NCT00899379	Organon and Co	Migraine Headache	April 1995	Phase 3
NCT00897104	Organon and Co	Migraine Headache	August 1995	Phase 3
NCT00897949	Organon and Co	Migraine Headache	March 1995	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H ₂ O : 100 mg/mL ( 255.45 mM ; Need ultrasonic)

DMSO : 50 mg/mL ( 127.72 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5545 mL	12.7724 mL	25.5447 mL
5 mM	0.5109 mL	2.5545 mL	5.1089 mL
10 mM	0.2554 mL	1.2772 mL	2.5545 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 50 mg/mL (127.72 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

* All of the co-solvents are available by MCE.

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.

Synonyms

1H-Indole-3-ethanamine, N,N-dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-, benzoate (1:1)

1H-Indole-3-ethanamine, N,N-dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-, monobenzoate

MK 462

Rizatriptan benzoate

Maxalt

Rizora

Rizact 5

Ritza