Cat. No. Name Size Price Add Cart
KI0876MAXALT (rizatriptan benzoate)10 mg$176
MAXALT (rizatriptan benzoate)50 mg$592
MAXALT (rizatriptan benzoate)100 mg$1072

Chemical Characteristic

Product NameMAXALT (rizatriptan benzoate)
SynonymsRizatriptan, Rizaliv, Rizalt, MK-462, L-705126
CAS No.145202-66-0
Molecular Weight 391.47
FormulaC22H25N5O2
Chemical Structure

Biological activities

Maxalt is a dual 5-HT 1D/1B receptor agonist. The IC50s of maxalt are 7 and 2 nM against 5-HT1B and 5-HT1D receptor, respectively. Maxalt potently and selectively binds to 5-HT(1B/1D) subtypes. Maxalt provides faster freedom from pain. Maxalt reduces nausea to a greater extent than oral sumatriptan.[1] Maxalt significantly decreases electrically stimulated dural vasodilation. Maxalt also significantly prevents dural plasma protein extravasation produced by high intensity electrical stimulation of the trigeminal ganglion. Maxalt inhibits the release of sensory neuropeptides from perivascular trigeminal nerves to prevent neurogenic vasodilation and extravasation in the dura mater.[2] Maxalt is mainly metabolized by MAO-A.[3] Maxalt selectively constricts isolated human middle meningeal arteries. Maxalt penetrates the blood閳ユ彽rain barrier and has significant inhibitory effects on durally mediated nociceptive responses in the central nerve system.[4]

References

[1] Wellington K, et al. Rizatriptan: an update of its use in the management of migraine. Drugs. 2002, 62(10): 1539-1574. 閵嗏偓閵嗏偓
[2] Williamson DJ, et al. The novel anti-migraine agent rizatriptan inhibits neurogenic dural vasodilation and extravasation. Eur J Pharmacol. 1997, 328(1): 61-64. 閵嗏偓閵嗏偓
[3] Iwasa T, et al. An in vitro interethnic comparison of monoamine oxidase activities between Japanese and Caucasian livers using rizatriptan, a serotonin receptor 1B/1D agonist, as a model drug. Br J Clin Pharmacol. 2003, 56(5): 537-544. 閵嗏偓閵嗏偓
[4] Cumberbatch MJ, et al. Rizatriptan has central antinociceptive effects against durally evoked responses. Eur J Pharmacol. 1997, 328(1): 37-40. 閵嗏偓閵嗏偓

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