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Metergoline

$30$145

Products Details

Product Description

– Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na+ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation[1][2][3].

Web ID

– HY-B1033

Storage Temperature

– -20°C, 3 years (Powder)

Shipping

– Blue Ice

Applications

– Neuroscience-Neuromodulation

Molecular Formula

– C25H29N3O2

References

– [1]Antony R Knight, et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23.|[2]Jessica A. Knight, et al. Pharmacological Analysis of the Novel, Rapid, and Potent Inactivation of the Human 5-Hydroxytryptamine7 Receptor by Risperidone, 9-OH-Risperidone, and Other Inactivating Antagonists. Mol Pharmacol. 2009 Feb; 75(2): 374-380.|[3]Jun-ho Lee, et al. Metergoline inhibits the neuronal Nav1.2 voltage-dependent Na+ channels expressed in Xenopus oocytes. Acta Pharmacol Sin. 2014 Jul; 35(7): 862-868.|[4]P K Eide, et al. The behavioural response to intrathecal serotonin is changed by acute but not by repeated treatment with zimelidine or metergoline. Pharmacol Toxicol. 1991 Nov;69(5):361-4.

CAS Number

– 17692-51-2

Molecular Weight

– 403.52

Compound Purity

– 99.89

SMILES

– O=C(OCC1=CC=CC=C1)NC[C@H](C[C@@]23[H])CN(C)[C@]2([H])CC4=CN(C)C5=CC=CC3=C54

Clinical Information

– Launched

Research Area

– Neurological Disease

Solubility

– DMSO : 66.67 mg/mL (ultrasonic)

Target

– 5-HT Receptor;Dopamine Receptor;Sodium Channel

Isoform

– 5-HT2 Receptor;5-HT7 Receptor

Pathway

– GPCR/G Protein;Membrane Transporter/Ion Channel;Neuronal Signaling

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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