Zolmitriptan

Catalog No.S1649

For research use only.

Zolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.

Zolmitriptan  Chemical Structure

CAS No. 139264-17-8

Selleck's Zolmitriptan has been cited by 1 Publication

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Biological Activity

Description Zolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.
Targets
5-HT [1]
In vitro

Zolmitriptan produces concentration-dependent contractions of primate basilar artery and human epicardial coronary artery rings. Zolmitriptan displays high affinity at human recombinant 5-HT1D (formerly 5-HT1D alpha) and 5-HT1B (formerly 5-HT1D beta) receptors in transfected CHO-K1 cell membranes. [1] Zolmitriptan increases I(K) in a concentration-dependent manner (maximum increase 16.3%) with a pD(2) value of 7.03 in C6 glioma cells expressing recombinant human 5-HT(1B) receptor. Zolmitriptan-induced increases in I(K) are prevented by the calcium chelator, EGTA (5 mM) when included in the patch pipette in C6 cells expressing cloned human 5-HT(1B) receptors. [2]

In vivo Zolmitriptan (3-30 mg/kg, i.v.) administrated ten minutes before unilateral electrical stimulation of the trigeminal ganglion causes a dose-dependent inhibition of [125I]-albumin extravasation within the ipsilateral dura mater in anaesthetized guinea-pigs. [1] Zolmitriptan (10-1000 mg/kg, i.v.) selectively reduces arteriovenous-anastomotic (AVA) conductance producing a maximum decrease of 92.5%. Zolmitriptan also produces a modest reduction in extra-cerebral conductance (23.9% maximum reduction at 30 mg/kg, i.v.), but is without effect on cerebral conductance. Zolmitriptan (1-30 mg/kg, i.v.) produces dose-dependent decreases in ear microvascular conductance (15% to 60%) which mirror decreases in carotid arterial conductance in anaesthetised cats. [3] Zolmitriptan exerts behaviorally specific anti-aggressive effects in mice. Zolmitriptan also decreases alcohol-heightened aggression with equal efficacy in mice. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 58 mg/mL
(201.83 mM)
Ethanol 58 mg/mL
(201.83 mM)
Water Insoluble

Chemical Information

Molecular Weight 287.36
Formula

C16H21N3O2

CAS No. 139264-17-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CCC1=CNC2=C1C=C(C=C2)CC3COC(=O)N3

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05019430 Recruiting Drug: Cocaine|Drug: Placebo oral capsule|Drug: Zolmitriptan Cocaine Use Disorder William Stoops|National Institute on Drug Abuse (NIDA)|University of Kentucky October 15 2021 Early Phase 1
NCT01085123 Completed Drug: Rapimelt|Drug: [11C]AZ10419369 Migraine AstraZeneca May 2010 Phase 1
NCT00637286 Completed Drug: Zolmitriptan Migraine AstraZeneca July 2004 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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