Almotriptan-d3 benzoate
Almotriptan-d3 benzoate (PNU180638 free base-d3) is deuterated labeled Almotriptan benzoate. Almotriptan benzoate is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan benzoate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan benzoate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan benzoate can be used in research related to migraine.
For research use only. We do not sell to patients.
- Formula: C24H28D3N3O4S
- Molecular Weight:460.60
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT1B Receptor |
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 154323-57-6
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Appearance Solid
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Molecular Weight 460.60
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Formula C24H28D3N3O4S
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SMILES
O=C(O)C1=CC=CC=C1.CN(CCC2=CNC3=C2C=C(C=C3)CS(=O)(N4CCCC4)=O)C([2H])([2H])[2H]
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Synonyms
PNU180638 free base-d3 benzoate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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]. Bou J, et al. Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine. Eur J Pharmacol, 2000. 410(1): p. 33-41. [Content Brief]
[3]. Gras J, et al. Safety profile of almotriptan, a new antimigraine agent. Effects on central nervous system, renal function and respiratory dynamics. Arzneimittelforschung, 2001. 51(9): p. 726-32. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)