Mepyramine-d2
Mepyramine-d2 (Pyrilamine-d2) is the d2-labeled Mepyramine (HY-118807). Mepyramine (Pyrilamine) is a selective histamine H1 receptor antagonist and KCNQ channel inhibitor, with an IC50 of 12.5 μM against KCNQ2/Q3. Mepyramine 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 can be used in studies related to seizures, convulsions, allergic asthma and morphine physical dependence.
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- Formule: C17H21D2N3O
- Masse moléculaire:287.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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H1 Receptor |
KCNQ2/Q3 12.5 μM (IC50) |
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled CAS 91-84-9
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Masse moléculaire 287.40
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Formule C17H21D2N3O
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SMILES
CN(CCN(C1=NC=CC=C1)CC2=CC([2H])=C(C([2H])=C2)OC)C
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Synonyms
Pyrilamine-d2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Ovalbumin-Induced Allergic Airway Inflammation
Ovalbumin-induced allergic airway inflammation is a mouse model in which systemic sensitization to ovalbumin, usually with aluminum hydroxide adjuvant, is followed by airway ovalbumin challenge to induce allergic airway inflammation, eosinophil recruitment, mucus production, serum antigen-specific IgE, Th2 cytokine responses, and airway hyperresponsiveness to methacholine. The model is used to study allergen-driven airway inflammation and asthma-like immune responses, but it does not reproduce every feature of human asthma. The main readouts are bronchoalveolar lavage fluid cellularity, lung histopathology, airway hyperresponsiveness, serum OVA-specific IgE, and cytokines such as IL-4, IL-5, and IL-13 in bronchoalveolar lavage fluid or lung samples. Eosinophilia and Th2 cytokines reflect allergic type 2 inflammation, while methacholine responsiveness provides a functional airway-reactivity endpoint.
Pureté et documentation
Références
[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-d2 Related Classifications
HY-118807S Related Classifications
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