Mepyramine maleate
Based on 2 publication(s) in Google Scholar
Mepyramine maleate (Pyrilamine maleate) is a selective histamine H1 receptor antagonist and KCNQ channel inhibitor, with an IC50 of 12.5 μM against KCNQ2/Q3. Mepyramine maleate shows no activity against allergic asthma in mice when used alone, but modulates the effect of JNJ 7777120 (HY-13508) on allergic asthma in mice; it inhibits the development of morphine physical dependence and increases histamine levels in mouse brains. Mepyramine maleate can be used in studies related to seizures, convulsions, allergic asthma and morphine physical dependence.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 59-33-6
- Formula: C21H27N3O5
- Molecular Weight:401.46
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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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Publications Citing Use of MedChemExpress (MCE) Mepyramine maleate
MoreAll Histamine Receptor Isoforms
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Biological Activity
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H1 Receptor |
KCNQ2/Q3 12.5 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
3.3 nM
Compound: pyrilamine
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Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
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[PMID: 23403082] |
| HEK293 | IC50 |
1.4 nM
Compound: Pyrilamine
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Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
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[PMID: 27876250] |
| HEK293 | IC50 |
1.9 nM
Compound: Pyrilamine
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Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
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[PMID: 27997171] |
| RBL-2H3 | IC50 |
0.0815 μM
Compound: 5i
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Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced mast cell degranulation preincubated with compound for 30 mins and then treated with C48/80 for 1 hr by neutral red dye based method
Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced mast cell degranulation preincubated with compound for 30 mins and then treated with C48/80 for 1 hr by neutral red dye based method
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[PMID: 31703894] |
| RBL-2H3 | IC50 |
0.0926 μM
Compound: 5i
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Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced histamine release preincubated with compound for 30 mins followed by C48/80 stimulation for 1 hr
Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced histamine release preincubated with compound for 30 mins followed by C48/80 stimulation for 1 hr
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[PMID: 31703894] |
| RBL-2H3 | IC50 |
0.132 μM
Compound: 5i
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Antiallergic activity in IgE/Ag-stimulated rat RBL2H3 cells assessed as inhibition of HSA-induced beta-hexosaminidase release preincubated with compound for 30 mins and then stimulated with HSA for 15 mins followed by incubation with P-nitrophenyl-N-acety
Antiallergic activity in IgE/Ag-stimulated rat RBL2H3 cells assessed as inhibition of HSA-induced beta-hexosaminidase release preincubated with compound for 30 mins and then stimulated with HSA for 15 mins followed by incubation with P-nitrophenyl-N-acety
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[PMID: 31703894] |
maleate of mepyramine (100 μM) potently and reversibly inhibits heterologously expressed KCNQ2/Q3 channels in HEK293 cells, with an IC50 of 12.5 μM, and alters channel gating kinetics and voltage-dependent activation in a voltage-dependent manner[1].
Mepyramine maleate inhibits homologous KCNQ1, KCNQ2, KCNQ3, KCNQ4 channels and heterologous KCNQ3/Q5 channels in HEK293 cells, with differential inhibitory potency; it exhibits the strongest activity against KCNQ3/Q5 (IC50 = 4.2 μM) and KCNQ3 (IC50 = 9.1 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pyrilamine (mepyramine) (50 mg/kg; i.p.; single dose) administered at the start of morphine dependence induction in WHT/Ht mice inhibits the development of morphine physical dependence (requiring 34.5-fold higher naloxone dose to precipitate 50% withdrawal jumping) without affecting morphine tolerance, and increases brain histamine levels by 25-37%[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (female, 8 weeks old, acclimatized for ≥2 weeks prior to experiments)[2]
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Dosage:20 mg/kg
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Administration:s.c.; 30 minutes before each ovalbumin exposure (provocation phase); 30 minutes before and 2 hours after each ovalbumin injection (sensitization phase)
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Result:Showed no significant reduction in BAL-fluid eosinophil numbers, no effect on lung tissue inflammatory infiltration scores, and no change in serum anti-OVA IgE, IL-13, or IL-5 concentrations relative to DMSO controls when administered during provocation.
Showed no significant reduction in BAL-fluid eosinophil numbers, reduced lung tissue inflammatory infiltration scores relative to DMSO controls, and no change in serum anti-OVA IgE, IL-13, or IL-5 concentrations relative to DMSO controls when administered during sensitization.
Inhibited JNJ 7777120-induced reductions in BAL-fluid eosinophil numbers and serum anti-OVA IgE concentrations when co-administered during provocation.
Enhanced JNJ 7777120-induced reductions in BAL-fluid eosinophil numbers and lung inflammatory infiltration scores, and significantly reduced serum IL-13 and IL-5 concentrations relative to DMSO controls when co-administered during sensitization.
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Animal Model:WHT/Ht (either sex, 25 to 40 g, morphine dependence induced via subcutaneous implantation of 7 mg morphine sulphate-impregnated molecular sieve pellets)[4]
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Dosage:50 mg/kg
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Administration:i.p.; single dose
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Result:Increased brain histamine levels 24 hours post-treatment: Non-tolerant mepyramine-treated mice had 25% higher brain histamine than non-tolerant controls; tolerant mepyramine-treated mice had 37% higher brain histamine than tolerant controls.
Brain histamine was 16% higher in tolerant mepyramine-treated mice than non-tolerant mepyramine-treated mice.
All increases were statistically significant.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 59-33-6
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Appearance Solid
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Molecular Weight 401.46
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Formula C21H27N3O5
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Color White to off-white
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SMILES
CN(C)CCN(CC1=CC=C(OC)C=C1)C2=NC=CC=C2.O=C(O)/C=C\C(O)=O
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Synonyms
Pyrilamine maleate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Eur J Pharmacol
The role of heterodimers formed by histamine H3 receptors and dopamine D1 receptors on the methamphetamine-induced conditioned place preference. [Abstract]2024 Oct 15:981:176866. PMID: 39089461 -
Pharmacol Res Perspect
Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats. [Abstract]2021 Oct;9(5):e00879. PMID: 34628723
Solvent & Solubility
DMSO : ≥ 100 mg/mL (249.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (124.55 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.5 mg/mL (6.23 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.23 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (249.09 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Liu B, et al. Antihistamine mepyramine directly inhibits KCNQ/M channel and depolarizes rat superior cervical ganglion neurons. Neuropharmacology. 2008;54(4):629-639. [Content Brief]
[2]. Beermann S, et al. Opposite effects of mepyramine on JNJ 7777120-induced amelioration of experimentally induced asthma in mice in sensitization and provocation. PLoS One. 2012;7(1):e30285. [Content Brief]
[3]. Dirikolu L, et al. Pyrilamine in the horse: detection and pharmacokinetics of pyrilamine and its major urinary metabolite O-desmethylpyrilamine. J Vet Pharmacol Ther. 2009;32(1):66-78. [Content Brief]
[4]. Hui KS, et al.The effect of mepyramine on the development of morphine tolerance and physical dependence in mice. Life Sci. 1975 Sep 15;17(6):891-9. [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 (sealed storage, away from moisture and light). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.4909 mL | 12.4545 mL | 24.9091 mL | 62.2727 mL |
| 5 mM | 0.4982 mL | 2.4909 mL | 4.9818 mL | 12.4545 mL | |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.4909 mL | 6.2273 mL | |
| 15 mM | 0.1661 mL | 0.8303 mL | 1.6606 mL | 4.1515 mL | |
| 20 mM | 0.1245 mL | 0.6227 mL | 1.2455 mL | 3.1136 mL | |
| 25 mM | 0.0996 mL | 0.4982 mL | 0.9964 mL | 2.4909 mL | |
| 30 mM | 0.0830 mL | 0.4152 mL | 0.8303 mL | 2.0758 mL | |
| 40 mM | 0.0623 mL | 0.3114 mL | 0.6227 mL | 1.5568 mL | |
| 50 mM | 0.0498 mL | 0.2491 mL | 0.4982 mL | 1.2455 mL | |
| 60 mM | 0.0415 mL | 0.2076 mL | 0.4152 mL | 1.0379 mL | |
| 80 mM | 0.0311 mL | 0.1557 mL | 0.3114 mL | 0.7784 mL | |
| 100 mM | 0.0249 mL | 0.1245 mL | 0.2491 mL | 0.6227 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Mepyramine maleate Related Classifications
HY-B1281 Related Classifications
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