1190043-69-6
Chemical Structure
Naratriptan-d3
Synonym(s): GR-85548A-d3-1
- CAS No.: 1190043-69-6
- Formula:C17H22D3N3O2S
- Molecular Weight:338.48
IUPAC Name: N-methyl-2-(3-(1-(methyl-d3)piperidin-4-yl)-1H-indol-5-yl)ethane-1-sulfonamide
InChIKey: AMKVXSZCKVJAGH-BMSJAHLVSA-N
SMILES: CNS(CCC1=CC=C2NC=C(C3CCN(CC3)C([2H])([2H])[2H])C2=C1)(=O)=O
Biological Activity: Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan (HY-B0197). Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan 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 also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms[1][2][3][4][5].
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Naratriptan-d3 | Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan (HY-B0197). Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan 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 also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms. | |||||||||||||||||||||
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Naratriptan | 99.81% | Naratriptan is an orally active and selective 5-HT1B/1D receptor agonist. Naratriptan 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 also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms. | ||||||||||||||||||||
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References
- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
- [2]. 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]
- [3]. 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]
- [4]. Connor HE, et al. Naratriptan: biological profile in animal models relevant to migraine. Cephalalgia. 1997 May;17(3):145-52. [Content Brief]
- [5]. 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]
