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Art. -Nr.: HY-W985814

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Nordimaprit

Nordimaprit is a reversible, non-competitive H3 receptor antagonist with a pK_i value of 5.94. Nordimaprit exhibits essentially no activity against H1 receptors and only weak agonistic activity against H2 receptors. Nordimaprit induces selective chemotaxis of eosinophils in rabbit eyes, triggering severe eosinophilic uveitis and ocular symptoms such as corneal edema, opacity, and inflammation. Nordimaprit reduces melanin content and inhibits tyrosinase activity, and exerts toxic effects on melanoma cells. Nordimaprit can be used in studies related to anterior uveitis and melanoma.

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CAS. Nr.: 17124-82-2
Formel: C₅H₁₃N₃S
Molecular Weight:147.24

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Please store the product under the recommended conditions in the Certificate of Analysis.

Nordimaprit Chemical Structure

CAS. Nr.: 17124-82-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
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Biologische Aktivität

Beschreibung

In Vitro

Nordimaprit binds to H₃ binding sites in rat brain cortex homogenates with a pK_i of 5.94, showing no differentiation between H₃A and H₃B binding site subtypes^[2].
Nordimaprit (0.5-10 μM; 110 min) acts as a reversible noncompetitive H₃ receptor antagonist in mouse brain cortex slices, reducing both the maximum inhibitory effect and potency of histamine with an apparent pD'₂ of 5.55^[2].
Nordimaprit (2 μM; 30 min) binds reversibly to presynaptic H₃ receptors in mouse brain cortex slices, as pre-exposure to the compound does not persistently reduce histamine's inhibitory activity^[2].
Nordimaprit (50 μM; 4 days) reduces melanin content to 72.31% and tyrosinase activity to 61% of control levels in human melanoma MM418 cells^[3].
Nordimaprit (0.03-1 mM; 48-66 h) inhibits Con A-induced activation of human peripheral blood mononuclear lymphocytes with an IC₅₀ of 0.03 mM, with cell mortality increasing in a dose-dependent manner alongside activation inhibition^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Nordimaprit (0.21 M; topical administration; 3 times daily; for more than 12 consecutive days) induces severe anterior segment eosinophilic uveitis in the eyes of all treated pigmented and albino rabbits. Pretreatment with Proparacaine (HY-66012A) or co-administration with Cimetidine (HY-14289) accelerates disease onset and produces unique ocular effects including a fibrinous aqueous humor reaction and mydriasis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Dutch Belted (pigmented); albino^[1]
Dosage:

0.21 M
Administration:

topical; three times daily; 12+ consecutive days; continued for an additional 48 hours if uveitis developed
Result:

Induced eosinophil uveitis in 5 of 5 treated eyes with onset at 5-10 days when administered alone.
Induced eosinophil uveitis in 5 of 5 treated eyes with onset at 2-3 days when administered with proparacaine.
Induced eosinophil uveitis in 5 of 5 treated eyes with onset at 2-3 days when administered with proparacaine and cimetidine.
Produced severe corneal opacification, a marked fibrinoid response in the aqueous humor, either transient miosis followed by marked mydriasis or direct marked mydriasis, and loss of intact iris stromal melanocytes.
Maintained peripheral blood eosinophil counts at 2-3% before, during, and after treatment.

Chemical Information

CAS. Nr. 17124-82-2
Molecular Weight 147.24
Formel C₅H₁₃N₃S
SMILES

N=C(SCCN(C)C)N
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Mindel JS, et al. Eosinophil chemotaxis and anterior uveitis from topical dimaprit and nordimaprit. Investigative ophthalmology & visual science. 1986 Oct;27(10):1504-11.

[2]. Kathmann M, et al. Nordimaprit, homodimaprit, clobenpropit and imetit: affinities for H3 binding sites and potencies in a functional H3 receptor model. Naunyn-Schmiedeberg's archives of pharmacology. 1993 Nov;348(5):498-503.

[3]. Fechner GA, et al. Inhibition of melanogenesis in human melanoma cells by novel analogues of the partial histamine (H2) agonist nordimaprit. Biochemical pharmacology. 1993 Jul 06;46(1):47-54.

[4]. Dale MM, et al. A comparison of dimaprit, nordimaprit, methylamine and chloroquine as inhibitors of mitogen-induced lymphocyte activation. British journal of pharmacology. 1984 Sep;83(1):293-8.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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