Zolmitriptan - Moligand™, 10mM in DMSO , Serotonin 1d (5-HT1d) receptor agonist, CAS No.139264-17-8, Serotonin 1d (5-HT1d) receptor agonist

CAS: 139264-17-8 Cat. No.: Z407928 Fórmula: C₁₆H₂₁N₃O₂ Peso molecular: 287.36 Número CE: 629-919-0 PubChem CID: 60857

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(4S)​-4-​[[3-​[2-​(dimethylamino)​ethyl]​-​1H-​indol-​5-​yl]​methyl]​-​2-​oxazolidinone

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

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

cell lines：HEK-293 cells expressing the human 5-HT2B receptor

Concentrations：

Incubation Time：

Powder Purity:≥100%

Specifications

Sinónimos

(4S)​-4-​[[3-​[2-​(dimethylamino)​ethyl]​-​1H-​indol-​5-​yl]​methyl]​-​2-​oxazolidinone

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

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

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Grau

Moligand™

Tipo de ação

AGONIST

Mecanismo de ação

Serotonin 1d (5-HT1d) receptor agonist

Propriedades do produto

• ALogP: 2.2

Nomes e identificadores

• SMILES isoméricas: CN(C)CCC1=CNC2=C1C=C(C=C2)C[C@H]3COC(=O)N3
• WGK Alemanha: 3
• RTECS: RQ2707000
• PubChem CID: 60857
• Peso molecular: 287.36

Alvos associados (humanos)

HTR1B Tclin 5-hydroxytryptamine receptor 1B (5 Activities)

Discover Target: HTR1B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1E Tchem 5-hydroxytryptamine receptor 1E (1 Activities)

Discover Target: HTR1E

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1D Tclin 5-hydroxytryptamine receptor 1D (6 Activities)

Discover Target: HTR1D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A (3 Activities)

Discover Target: HTR1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propriedades químicas e físicas

• Rotação específica [α]: -4° (C=1,MeOH)
• Ponto de fusão (°C): 135-137°C

Referências

1. Xiaohui Zhang, Yule Wang, Kai Zhang, Hongda Sheng, Yuhan Wu, Huimin Wu, Yingchao Wang, Jianli Guan, Qingfen Meng, Huahuan Li, Zhenhao Li, Guanwei Fan, Yi Wang.  (2021)  Discovery of tetrahydropalmatine and protopine regulate the expression of dopamine receptor D2 to alleviate migraine from Yuanhu Zhitong formula.  PHYTOMEDICINE,      [PMID:34419734] [10.1016/j.phymed.2021.153702]

Perguntas frequentes

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 139264-17-8, the molecular formula is C16H21N3O2, and the molecular weight is 287.36 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.