2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Membrane Transporter/Ion Channel
  3. Histamine Receptor Potassium Channel
  4. Mepyramine hydrochloride

Mepyramine hydrochloride  (Synonyms: Pyrilamine hydrochloride)

Cat. No.: HY-118807A
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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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Mepyramine hydrochloride

Mepyramine hydrochloride Chemical Structure

CAS No. : 6036-95-9

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Mepyramine hydrochloride Related Antibodies

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Description

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[1][2][3][4].

IC50 & Target[1]

H1 Receptor

 

KCNQ2/Q3

12.5 μM (IC50)

In Vitro


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.

Mepyramine hydrochloride Related Antibodies
Parmacokinetics
Species Dose Route T1/2 (Distribution) T1/2β AUC0-inf Vdss MRT Bioavailability Tmax Cmax
Horse[3] 0.52-0.66 mg/kg i.v. 0.308 h 1.67 h 297 ng·h/mL 1901 L 1.76 h / / /
Horse[3] 0.52-0.66 mg/kg p.o. / / 54.6 ng·h/mL / 1.48 h 18.4 % 0.44 h 36.6 ng/mL
In Vivo

Pyrilamine (20 mg/kg; s.c.) alone has minimal independent effect on murine allergic asthma parameters, but exerts phase-dependent modulation of JNJ 7777120 efficacy, inhibiting beneficial effects during provocation and enhancing beneficial effects during sensitization[2].
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.

Animal Model: Balb/c (female, 8 weeks old, acclimatized for ≥2 weeks prior to experiments)[2]
Dosage: 20 mg/kg
Administration: s.c.; 30 minutes before each ovalbumin exposure (provocation phase); 30 minutes before and 2 hours after each ovalbumin injection (sensitization phase)
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.
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]
Dosage: 50 mg/kg
Administration: i.p.; single dose
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.
Molecular Weight

321.84

Formula

C17H24ClN3O
CAS No.
SMILES

COC(C=C1)=CC=C1CN(CCN(C)C)C2=NC=CC=C2.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Mepyramine hydrochloride Related Classifications

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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:

Mepyramine6036-95-9PyrilamineHistamine ReceptorPotassium ChannelKcsAallergic asthmaseizuresWHT/Ht miceblood-brain barriermorphine physical dependenceconvulsionsKCNQ channelurticariaHEK293 cellshistamine H1 receptorInhibitorinhibitorinhibit

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