Naratriptan hydrochloride
Based on 2 publication(s) in Google Scholar
Naratriptan (GR-85548A) hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.69%
- CAS. Nr.: 143388-64-1
- Formel: C17H26ClN3O2S
- Molecular Weight:371.93
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Speicherung:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Naratriptan hydrochloride
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Biologische Aktivität
Beschreibung
IC50 & Target
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5-HT1B Receptor |
5-HT1 Receptor |
In Vitro
Naratriptan hydrochloride targets human recombinant 5-HT1B and 5-HT1D receptors with Ki of 0.47 nM and 0.69 nM, and EC50 of 4.4 nM and 23 nM, respectively; while for 5-HT1A, Ki=26 nM, EC50=79 nM[1].
Naratriptan hydrochloride targets 5-HT1B, 5-HT1D, and 5-HT1F with pKi of 8.7, 8.3, and 8.1, respectively[2].
Naratriptan hydrochloride can inhibit the discharge response of cat-derived nucleus tractus solitarius (NTS) cells that regulate vomiting by 54%; this activity suggests that Naratriptan hydrochloride has inhibitory activity on NTS in trigeminal nerve vessels and can be used in the study of migraine inhibition[2].
Naratriptan hydrochloride induces concentration-dependent contraction in isolated dog basilar artery and middle cerebral artery experiments, with EC50 of 0.11 M and 0.07 M, respectively[3].
Naratriptan hydrochloride induces contraction in isolated human epicardial coronary arteries with an EC50 value of 0.17 μM; the maximal contraction induced at this point is 33% of the maximal 5-HT response[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Naratriptan (10 mg/kg; oral; single dose) hydrochloride has an oral bioavailability of 71% in male Wistar rats. Naratriptan (0.5 mg/kg; oral; single dose) hydrochloride has an oral bioavailability of 95% in beagle dogs[3].
Contrary to the activity of μ-opioid receptor agonists, Naratriptan [(10, 30 μg/kg; intrathecal injection; single dose) or (10, 30 mg/kg; subcutaneous injection; single dose)] hydrochloride does not increase the latency of the tail flick response or hot plate response in mice in the tail flick test or hot plate test. Neither or Naratriptan (10, 30 mg/kg; subcutaneous injection; single dose) hydrochloride also does not increase the nociceptive paw pressure threshold in the paw pressure test in guinea pigs and rats[3].
Naratriptan (10 mg/mL; IV/iontophoresis; single dose) hydrochloride inhibits the responses of trigeminal nucleus caudalis neurons to sagittal sinus stimulation in the cat trigeminal neurovascular stimulation model, an effect that can be reversed by the 5-HT1B/1D receptor antagonists (5 mg/mL) SB224289 (HY-101105) and BRL15572 (HY-13200B)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 143388-64-1
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Appearance Solid
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Molecular Weight 371.93
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Formel C17H26ClN3O2S
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Color White to off-white
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SMILES
O=S(CCC1=CC2=C(NC=C2C3CCN(C)CC3)C=C1)(NC)=O.Cl
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Synonyms
GR-85548A hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Exp Med
2022 Aug 1;219(8):e20212307. PMID: 35796804 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 35 mg/mL (94.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 6.67 mg/mL (17.93 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 6.67 mg/mL (17.93 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (393 KB)
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- Français - FR (393 KB)
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- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Rhoden E, et al. Anti-poliovirus activity of protease inhibitor AG-7404, and assessment of in vitro activity in combination with antiviral capsid inhibitor compounds. Antiviral Res. 2013 May;98(2):186-91. [Content Brief]
[2]. Hoskin KL, et al. The 5-hydroxytryptamine1B/1D/1F receptor agonists eletriptan and naratriptan inhibit trigeminovascular input to the nucleus tractus solitarius in the cat. Brain Res. 2004 Feb 13;998(1):91-9. [Content Brief]
[3]. Connor HE, et al. Naratriptan: biological profile in animal models relevant to migraine. Cephalalgia. 1997 May;17(3):145-52. [Content Brief]
[4]. Donaldson C, et al. The role of 5-HT1B and 5-HT1D receptors in the selective inhibitory effect of naratriptan on trigeminovascular neurons. Neuropharmacology. 2002 Mar;42(3):374-85. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.6887 mL | 13.4434 mL | 26.8868 mL | 67.2170 mL |
| 5 mM | 0.5377 mL | 2.6887 mL | 5.3774 mL | 13.4434 mL | |
| 10 mM | 0.2689 mL | 1.3443 mL | 2.6887 mL | 6.7217 mL | |
| 15 mM | 0.1792 mL | 0.8962 mL | 1.7925 mL | 4.4811 mL | |
| DMSO | 20 mM | 0.1344 mL | 0.6722 mL | 1.3443 mL | 3.3608 mL |
| 25 mM | 0.1075 mL | 0.5377 mL | 1.0755 mL | 2.6887 mL | |
| 30 mM | 0.0896 mL | 0.4481 mL | 0.8962 mL | 2.2406 mL | |
| 40 mM | 0.0672 mL | 0.3361 mL | 0.6722 mL | 1.6804 mL | |
| 50 mM | 0.0538 mL | 0.2689 mL | 0.5377 mL | 1.3443 mL | |
| 60 mM | 0.0448 mL | 0.2241 mL | 0.4481 mL | 1.1203 mL | |
| 80 mM | 0.0336 mL | 0.1680 mL | 0.3361 mL | 0.8402 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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