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Metergoline

CAT: 0804-HY-B1033-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-B1033-01Size:5 mg
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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

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