2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. 5-HT Receptor Dopamine Receptor Sodium Channel
  4. Metergoline

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.

Metergoline Chemical Structure

Metergoline Chemical Structure

CAS No. : 17692-51-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 33 In-stock
Solution
10 mM * 1 mL in DMSO USD 33 In-stock
Solid
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10 mg USD 42 In-stock
50 mg USD 106 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Metergoline Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Metergoline

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

IC50 & Target[1][2]

5-HT2A Receptor

8.64 (pKi)

5-HT2B Receptor

8.75 (pKi)

5-HT2C Receptor

8.75 (pKi)

Human 5-HT7 Receptor

16 nM (Ki)

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 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.

Metergoline Related Antibodies
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).
Molecular Weight

403.52

Formula

C25H29N3O2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4782 mL 12.3910 mL 24.7819 mL
5 mM 0.4956 mL 2.4782 mL 4.9564 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.89%

SDS (393 KB)

COA (245 KB) HNMR (285 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

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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Metergoline Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Metergoline17692-51-25-HT ReceptorDopamine ReceptorSodium ChannelSerotonin Receptor5-hydroxytryptamine ReceptorNa channelsNa+ channelspsychoactiveaffectivedisorderprolactinhormoneregulationpremenstrualdysphoricInhibitorinhibitorinhibit

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