Metergoline
Based on 2 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 17692-51-2
- Formula: C25H29N3O2
- Molecular Weight:403.52
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Metergoline
MoreAll 5-HT Receptor Isoforms
MoreAll Dopamine Receptor Isoforms
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Biological Activity
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5-HT2A Receptor 8.64 (pKi) |
5-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
5-HT7 Receptor |
5-HT2B Receptor 8.75 (pKi) |
5-HT2C Receptor 8.75 (pKi) |
Human 5-HT7 Receptor 16 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| Astrocyte | EC50 |
3.285 μM
Compound: Metergoline
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Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
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[PMID: 17417631] |
| CHO | EC50 |
7.5 nM
Compound: metergoline
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Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells
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[PMID: 16562853] |
| CHO | IC50 |
16.6 μM
Compound: 1
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Cytotoxicity against CHO cells by MTT assay
Cytotoxicity against CHO cells by MTT assay
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10.1039/C3MD00310H |
| CHO-K1 | IC50 |
4.1 nM
Compound: metergoline
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Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHOK1 cells after 60 mins
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHOK1 cells after 60 mins
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[PMID: 23403082] |
Metergoline (3 μM) causes a 6.8±1.2 mV depolarizing shift of the steady-state activation curve of the Na+currents, and does not alter the inactivation curve[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male albino mice (25-40 g)[4]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection
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Result:Inhibited bites or scratches induced by 5-HT (2 μg).
Chemical Information
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CAS No. 17692-51-2
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Appearance Solid
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Molecular Weight 403.52
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Formula C25H29N3O2
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
The Locus Coeruleus-Periaqueductal Gray GABAergic Projection Regulates Comorbid Pain and Depression. [Abstract]2025 Apr 7:e2503739. PMID: 40192524 -
Solvent & Solubility
DMSO : 66.67 mg/mL (165.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4782 mL | 12.3910 mL | 24.7819 mL | 61.9548 mL |
| 5 mM | 0.4956 mL | 2.4782 mL | 4.9564 mL | 12.3910 mL | |
| 10 mM | 0.2478 mL | 1.2391 mL | 2.4782 mL | 6.1955 mL | |
| 15 mM | 0.1652 mL | 0.8261 mL | 1.6521 mL | 4.1303 mL | |
| 20 mM | 0.1239 mL | 0.6195 mL | 1.2391 mL | 3.0977 mL | |
| 25 mM | 0.0991 mL | 0.4956 mL | 0.9913 mL | 2.4782 mL | |
| 30 mM | 0.0826 mL | 0.4130 mL | 0.8261 mL | 2.0652 mL | |
| 40 mM | 0.0620 mL | 0.3098 mL | 0.6195 mL | 1.5489 mL | |
| 50 mM | 0.0496 mL | 0.2478 mL | 0.4956 mL | 1.2391 mL | |
| 60 mM | 0.0413 mL | 0.2065 mL | 0.4130 mL | 1.0326 mL | |
| 80 mM | 0.0310 mL | 0.1549 mL | 0.3098 mL | 0.7744 mL | |
| 100 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6195 mL |
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