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

Metergoline 

Cat. No.: HY-B1033 Purity: 99.74%
Handling Instructions

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 also is 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
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
50 mg USD 96 In-stock
Estimated Time of Arrival: December 31
100 mg USD 132 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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 also is a reversible neural Na+ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation[1][2][3].

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 do not alter the inactivation curve[3].

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].

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.

17692-51-2

SMILES

O=C(OCC1=CC=CC=C1)NC[[email protected]](C[[email protected]@]23[H])CN(C)[[email protected]]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 : 50 mg/mL (123.91 mM; Need ultrasonic)

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
10 mM 0.2478 mL 1.2391 mL 2.4782 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.74%

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Keywords:

Metergoline5-HT ReceptorDopamine ReceptorSodium ChannelSerotonin Receptor5-hydroxytryptamine ReceptorNa channelsNa+ channelspsychoactiveaffectivedisorderprolactinhormoneregulationpremenstrualdysphoricInhibitorinhibitorinhibit

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Metergoline
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HY-B1033
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