Metergoline

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].

Product Specifications

CAS Number

[17692-51-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

5-HT Receptor; Dopamine Receptor; Sodium Channel

Type

Reference compound

Related Pathways

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

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Metergoline.html

Purity

99.94

Solubility

DMSO : 66.67 mg/mL (ultrasonic)

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

Molecular Formula

C25H29N3O2

Molecular Weight

403.52

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.