Discontinued Product

Metergoline (Cat. No. 0590) has been withdrawn from sale for commercial reasons.
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 (4)
Reviews (1)
Literature (1)

Biological Activity for Metergoline

Metergoline is an antagonist at 5-HT1/5-HT2 with activity at 5-HT1D. Has moderate affinity for 5-HT6 and high affinity for 5-HT7.

Technical Data for Metergoline

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for Metergoline

References are publications that support the biological activity of the product.

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 sumatr. and metergoline at the human 5-HT1Dβ receptor in the action of sumatr. Eur.J.Pharmacol. 227 99 PMID: 1330643

Negri et al (1998) Respiratory and cardiovascular effects of the mu-opioid receptor agonist [Lys7]dermorphin in awake rats. Br.J.Pharmacol. 124 345 PMID: 9641552

View Related Products by Product Action

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Keywords: Metergoline, Metergoline supplier, moderate, affinity, 5-HT6, high, 5-HT7, 5-HT1, 5-HT2, antagonists, 5-HT1D, ligand, Serotonin, Receptors, 5-Hydroxytryptamine, 5-HT, Non-Selective, Non-selective, 0590, Tocris Bioscience

4 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 NE reuptake inhibition. Sci Rep 7 43137 PMID: 28230181

Lee et al (2014) Metergoline inhibits the neuronal Nav1.2 voltage-dependent Na(+) channels expressed in Xenopus oocytes. Acta Pharmacol Sin 35 862 PMID: 24909513

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

Chan et al (2016) A Miniaturized Screen of a Schistosoma mansoni Serotonergic G Protein-Coupled Receptor Identifies Novel Classes of Parasite-Selective Inhibitors. PLoS Pathog 12 e1005651 PMID: 27187180

Reviews for Metergoline

Average Rating: 1 (Based on 1 Review.)

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Could not dissolve for in vivo use.
By Anonymous on 06/17/2019
Assay Type: In Vivo
Species: Mouse

dissolved fine in DMSO, but came out of solution as soon as I added any saline. Would not stay in solution at even 50% DMSO in saline, it precipitated out into a fluffy white solid (picture attached). Also tried to dissolve in 1% ascorbic acid, and that didn't work either (1mg/ml). Also could not dissolve in 10% ascorbic acid (1mg/ml). I tried heating, vortexing, and sonicating with both and could not get it into solution. could not use with with my experiments

Tocris reply: We're sorry to hear that you have experienced problems with the solubility of Metergoline. We would like to make you aware of the following publication where metergoline 10 mg was solubilized in 1 ml of 45% w/v 2‐hydroxypropyl‐ beta ‐cyclodextrin in H2O and the solution lyophilized to form a fully soluble powder (Negri et al., 1998. PMID: 9641552). The powder (460 mg) was then dissolved in 30 ml of saline and injected in a volume of 1–6 ml kg−1 (s.c). We would like to offer a replacement vial if you no longer have any remaining material for attempting this solubilization method. If this is of interest, please contact us at

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

5-HT Receptors Scientific Review

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.