For research use only.
CAS No. 139264-17-8
Zolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.
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|Description||Zolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.|
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.  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. 
|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.  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.  Zolmitriptan exerts behaviorally specific anti-aggressive effects in mice. Zolmitriptan also decreases alcohol-heightened aggression with equal efficacy in mice. |
|In vitro||DMSO||58 mg/mL (201.83 mM)|
|Ethanol||58 mg/mL (201.83 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT05019430||Not yet recruiting||Drug: Cocaine|Drug: Placebo oral capsule|Drug: Zolmitriptan||Cocaine Use Disorder||William Stoops|National Institute on Drug Abuse (NIDA)|University of Kentucky||October 1 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|
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