Home Neuronal Signaling 5-HT Receptor agonist Zolmitriptan For research use only.

Zolmitriptan

Synonyms: BW-311C90

Zolmitriptan(BW-311C90) is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.

Zolmitriptan Chemical Structure

Zolmitriptan Chemical Structure

CAS: 139264-17-8

Selleck's Zolmitriptan has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 100%
100

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Biological Activity

Description Zolmitriptan(BW-311C90) 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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06074016 Completed Healthy Parc de Salut Mar|Food and Drug Administration (FDA) July 12 2023 Phase 1
NCT05019430 Recruiting Cocaine Use Disorder William Stoops|National Institute on Drug Abuse (NIDA)|University of Kentucky October 15 2021 Early Phase 1
NCT01085123 Completed Migraine AstraZeneca May 2010 Phase 1
NCT00637286 Completed Migraine AstraZeneca July 2004 Phase 4

Chemical lnformation & Solubility

Molecular Weight 287.36 Formula

C16H21N3O2
CAS No. 139264-17-8 SDF Download Zolmitriptan SDF
Smiles CN(C)CCC1=CNC2=C1C=C(C=C2)CC3COC(=O)N3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 58 mg/mL ( (201.83 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 58 mg/mL

Water : Insoluble


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