Metergoline

• 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].

• 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.

• Shipping Conditions :

  Blue Ice

• Storage Conditions :

  -20°C, 3 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Isoform :

  5-HT2 Receptor;5-HT7 Receptor; MUC3; α-1 microglobulin