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Cat.No. 0590 - Metergoline | C25H29N3O2 | CAS No. 17692-51-2
Description: 5-HT2 antagonist. Also 5-HT1 antagonist and 5-HT1D ligand. Has moderate affinity for 5-HT6 and high affinity for 5-HT7
Chemical Name: [(8β)-1,6-Dimethylergolin-8-yl)methyl]carbamic acid phenylmethyl ester
Citations (2)

Biological Activity

Antagonist at 5-HT1/5-HT2 with activity at 5-HT1D. Has moderate affinity for 5-HT6 and high affinity for 5-HT7.

Compound Libraries

Metergoline is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 403.52
Formula C25H29N3O2
Storage Store at RT
CAS Number 17692-51-2
PubChem ID 28693
Smiles [H][C@](CNC(OCC5=CC=CC=C5)=O)1C[C@@](C2=CC=CC3=C2C(C4)=CN3C)([H])[C@]4([H])N(C1)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 40.35 100

Preparing Stock Solutions

The following data is based on the product molecular weight 403.52. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.48 mL 12.39 mL 24.78 mL
5 mM 0.5 mL 2.48 mL 4.96 mL
10 mM 0.25 mL 1.24 mL 2.48 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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Product Datasheets

Safety Datasheet


References are publications that support the products' biological activity.

Aulakh et al (1992) Effects of various serotonin receptor subtype selective antagonists alone and on m-chlorophenylpiperazine-induced neuroendocrine changes in rats. J.Pharmacol.Exp.Ther. 263 588 PMID: 1432690

Bagdy et al (1992) Pharmacological characterization of serotonin receptor subtypes involved in vasopressin and plasma renin activity responses to serotonin agonists. Eur.J.Pharmacol. 210 285 PMID: 1535317

Miller et al (1992) Agonist activity of sumatriptan and metergoline at the human 5-HT1Dβ receptor in the action of sumatriptan. Eur.J.Pharmacol. 227 99 PMID: 1330643

If you know of a relevant reference for Metergoline, please let us know.

View Related Products by Product Action

View all Non-selective 5-HT2 Antagonists

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2 Citations for Metergoline

Citations are publications that use Tocris products. Selected citations for Metergoline include:

Wang (2017) Dezocine exhibits antihypersensitivity activities in neuropathy through spinal μ-opioid receptoractivation and norepinephrine reuptake inhibition. Sci Rep 7 43137 PMID: 28230181

Woo et al (2007) Neuregulin-1 enhances depolarization-induced GABA release. Neuron 54 599 PMID: 17521572

Do you know of a great paper that uses Metergoline from Tocris? If so please let us know.

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Literature in this Area


GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
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5-HT Receptors

5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.