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Purity: ≥98%
Naratriptan HCl (GR-85548A; GR85548A; Amerge; Naramig), the hydrochloride salt of naratriptan, is a triptan class of selective 5-HT₁ receptor subtype agonist used for the treatment of migraine headaches. was created and distributed by GSK, and tablets containing 2.5 mg are available. Naratriptan functions as a selective agonist of the 5-HT1 receptor subtype as its mode of action. Naratriptan is used to treat acute migraine attacks as well as the symptoms of migraine, which include intense, throbbing headaches that can occasionally be accompanied by light or sound sensitivity and nausea.
| Targets |
5-HT1 Receptor
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| Additional Infomation |
Naratriptan Hydrochloride is the hydrochloride salt form of naratriptan, a sulfonamide with selective serotonin (5-HT) 1 receptor agonistic activity and anti-migraine property. Naratriptan hydrochloride binds selectively and with high affinity to the 5-HT1D and 5-HT1B receptor subtypes. Activation of these 5-HT1D/B receptors located on intracranial blood vessels leads to vasoconstriction and provides relief of migraine headaches. Naratriptan hydrochloride may also exerts its effect by stimulation of 5-HT1D/1B receptors on sensory nerve endings in the trigeminal system thereby decreasing the release of pro-inflammatory neuropeptides.
See also: Naratriptan (has active moiety). |
| Molecular Formula |
C17H26CLN3O2S
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| Molecular Weight |
371.93
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| Exact Mass |
371.143
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| Elemental Analysis |
C, 54.90; H, 7.05; Cl, 9.53; N, 11.30; O, 8.60; S, 8.62
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| CAS # |
143388-64-1
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| Related CAS # |
Naratriptan; 121679-13-8; Naratriptan-d3 hydrochloride; 1190021-64-7
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| PubChem CID |
60875
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| Appearance |
White to off-white solid powder
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| Boiling Point |
541.3ºC at760mmHg
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| Melting Point |
234-236ºC
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| Flash Point |
281.2ºC
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| Vapour Pressure |
8.81E-12mmHg at 25°C
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| LogP |
4.28
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
483
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].S(C([H])([H])C([H])([H])C1C([H])=C([H])C2=C(C=1[H])C(=C([H])N2[H])C1([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])(N([H])C([H])([H])[H])(=O)=O
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| InChi Key |
AWEZYKMQFAUBTD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H25N3O2S.ClH/c1-18-23(21,22)10-7-13-3-4-17-15(11-13)16(12-19-17)14-5-8-20(2)9-6-14;/h3-4,11-12,14,18-19H,5-10H2,1-2H3;1H
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| Chemical Name |
N-methyl-2-[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]ethanesulfonamide;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2935.90.6000
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 6.67 mg/mL (17.93 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
Solubility in Formulation 2: 5%DMSO + 40%PEG300 + 5%Tween 80 + 50%ddH2O: 3.7mg/ml (9.95mM) (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6887 mL | 13.4434 mL | 26.8868 mL | |
| 5 mM | 0.5377 mL | 2.6887 mL | 5.3774 mL | |
| 10 mM | 0.2689 mL | 1.3443 mL | 2.6887 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01161667 | Completed | Drug: naratriptan hydrochloride | Migraine | Roxane Laboratories | September 2007 | Not Applicable |
| NCT01161654 | Completed | Drug: naratriptan hydrochoride | Migraine | Roxane Laboratories | August 2007 | Not Applicable |
| NCT01332383 | Completed | Drug: Naratriptan | Migraine Disorders | GlaxoSmithKline | May 2009 | N/A |
| NCT01376193 | Completed | Drug: Naratriptan | Migraine Disorders | GlaxoSmithKline | April 2009 | N/A |
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