Mepyramine hydrochloride
Based on 2 publication(s) in Google Scholar
Mepyramine hydrochloride (Pyrilamine hydrochloride) is a selective histamine H1 receptor antagonist and KCNQ channel inhibitor, with an IC50 of 12.5 μM against KCNQ2/Q3. Mepyramine hydrochloride 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 hydrochloride can be used in studies related to seizures, convulsions, allergic asthma and morphine physical dependence.
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- CAS No.: 6036-95-9
- 화학식: C17H24ClN3O
- 분자량:321.84
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Mepyramine hydrochloride
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Biological Activity
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H1 Receptor |
KCNQ2/Q3 12.5 μM (IC50) |
Hydrochloride 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 hydrochloride 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.
Chemical Information
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CAS No. 6036-95-9
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분자량 321.84
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화학식 C17H24ClN3O
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SMILES
COC(C=C1)=CC=C1CN(CCN(C)C)C2=NC=CC=C2.Cl
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Synonyms
Pyrilamine hydrochloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
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
순도&문서
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Mepyramine hydrochloride Related Classifications
HY-118807A Related Classifications
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