Art. -Nr.: HY-B1033

Metergoline

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pK_is of 8.64, 8.75 and 8.75 for 5-HT_2A, 5-HT_2B and 5-HT_2C, respectively. Metergoline is a high-affinity ligand for the h5-HT₇ receptor, with a K_i 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.

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Reinheit: 99.94%
CAS. Nr.: 17692-51-2
Formel: C₂₅H₂₉N₃O₂
Molecular Weight:403.52

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Metergoline Chemical Structure

CAS. Nr.: 17692-51-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

5-HT_2A Receptor

8.64 (pKi)

5-HT_2A Receptor

5-HT_2B Receptor

5-HT_2C Receptor

5-HT₇ Receptor

5-HT_2B Receptor

8.75 (pKi)

5-HT_2C Receptor

8.75 (pKi)

Human 5-HT₇ Receptor

16 nM (Ki)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Astrocyte	EC₅₀	3.285 μM Compound: Metergoline	Antiproliferative activity against mouse astrocyte cells by MTT assay Antiproliferative activity against mouse astrocyte cells by MTT assay	[PMID: 17417631]
CHO	EC₅₀	7.5 nM Compound: metergoline	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	[PMID: 16562853]
CHO	IC₅₀	16.6 μM Compound: 1	Cytotoxicity against CHO cells by MTT assay Cytotoxicity against CHO cells by MTT assay	10.1039/C3MD00310H
CHO-K1	IC₅₀	4.1 nM Compound: metergoline	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	[PMID: 23403082]

In Vitro

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.

In Vivo

Metergoline (5 mg/kg; i.p.) completely blocks the response to intrathecal 5-HT (2 μg)^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male albino mice (25-40 g)^[4]
Dosage:

5 mg/kg
Administration:

Intraperitoneal injection
Result:

Inhibited bites or scratches induced by 5-HT (2 μg).

Chemical Information

CAS. Nr. 17692-51-2
Appearance Solid
Molecular Weight 403.52
Formel C₂₅H₂₉N₃O₂
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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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
SSRN

2023 Dec 27.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4782 mL

12.3910 mL

24.7819 mL

5 mM

0.4956 mL

2.4782 mL

4.9564 mL

10 mM

0.2478 mL

1.2391 mL

2.4782 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Metergoline

2 Cited Publications

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Metergoline

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Publications Citing Use of MedChemExpress (MCE) Metergoline

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Metergoline Related Classifications

HY-B1033 Related Classifications