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KI0910Zolmitriptan10 mg$144
Zolmitriptan25 mg$272

Chemical Characteristic

Product NameZolmitriptan
Synonyms311 C90,Zomig
CAS No.139264-17-8
Molecular Weight 287.36
FormulaC16H21N3O2
Chemical Structure

Biological activities

Zolmitriptan is a new generation and highly selective 5-HT1B/1D receptor agonist used in the acute oral treatment of migraine.[1]Zolmitriptan is a structural analogue of serotonin (5-HT). Zolmitriptan has strong affinities for the 5-HT1B and 5-HT1D receptors with Ki of 5.01 and 0.63 nM, respectively. [2] Administered zolmitriptan can inhibit evoked trigeminovascular activity within the trigeminal nucleus. Intravenous zolmitriptan inhibits release of both calcitonin gene-related peptide (CGRP) and vasoactive intestinal polypeptide (VIP) provoked by trigeminal ganglion stimulation. [3] Zolmitriptan potently stimulates the inositol phosphate formation at ca 5-HT1D receptors with an EC50 of 4.9 nM. [4] Zolmitriptan, in rats after intravenous and intracerebral administration, at 3.2 mg/kg, decreases 5-HT levels by about 35%.[5]

Protocols

Zolmitriptan is dissolved in DMSO. [1]

References

[1] Yu L, et al. Transport characteristics of zolmitriptan in a human intestinal epithelial cell line Caco-2. J Pharm Pharmacol. 2007, 59(5): 655-660. 閵嗏偓閵嗏偓
[2] Patel SR, et al. Controlled non-invasive transdermal iontophoretic delivery of zolmitriptan hydrochloride in vitro and in vivo. Eur J Pharm Biopharm. 2009, 72(2): 304-309. 閵嗏偓閵嗏偓
[3] Goadsby PJ, et al. Inhibition of trigeminal neurons by intravenous administration of the serotonin (5HT) 1B/D receptor agonist zolmitriptan (311C90): are brain stem sites therapeutic target in migraine? Pain. 1996, 67(2-3): 355-359. 閵嗏偓閵嗏偓
[4] Wurch T, et al. Coupling of canine serotonin 5-HT1B and 5-HT1D receptor subtypes to the formation of inositol phosphates by dual interactions with endogenous Gi/o and recombinant G15 proteins. J Neurochem. 2000, 75(3): 1180-1189. 閵嗏偓閵嗏偓
[5] Johnson DE, et al. Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001, 425(3): 203-210. 閵嗏偓閵嗏偓

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