Pheniramine (Synonyms: Prophenpyridamine; Tripoton; Pheniramine solution)

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Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects.

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Pheniramine Chemical Structure

CAS No. : 86-21-5

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Other In-stock Forms of Pheniramine:

Pheniramine maleate

Other Forms of Pheniramine:

Pheniramine maleate In-stock

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

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Description

IC₅₀ & Target

H₁ Receptor

1.01 mM (IC₅₀)

In Vitro

Pheniramine inhibits CYP2D6, the specific P450-isozymes, to delay metabolic time and prolong antihistaminic effects^[1].
Pheniramine inhibits Ca²⁺ influx into BC3H-1 cells by inhibiting histamine with an IC₅₀ value of 1.01 mM and regulates cellular Ca²⁺ transmembrane action^[2].
Pheniramine (0.5, 1.0 mM; 24 h) induces cell apoptosis in human T-cell acute lymphoblastic leukemia cell lines^[3].
Pheniramine (1 μM-1 mM; 12-48 h) inhibits cell proliferation in a time-dependent manner and shows inhibitory concentration IC₅₀s of 550 μM (CCRF-CEM cells) and 420 μM (Jurkat cells), respectively^[3].

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

Apoptosis Analysis^[3]

Cell Line:	Human T-cell acute lymphoblastic leukemia cell lines: CCRF-CEM and Jurkat ALL
Concentration:	0.5, 1.0 mM
Incubation Time:	24 hours
Result:	Induced cells apoptosis with chromatin condenses and marginalizes, and nuclear debris spreaded into the cytoplasm.

Cell Viability Assay^[3]

Cell Line:	Human T-cell acute lymphoblastic leukemia cell lines: CCRF-CEM and Jurkat ALL
Concentration:	1 μM-1 mM
Incubation Time:	12, 24, 48 hours
Result:	Inhibited cell proliferation and survival in a time- and dose-dependent manner.

In Vivo

Pheniramine (1.75 μM; i.t.) exerts local anesthesia effect and results spinal block in rats^[4].

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

Animal Model:	Sprague–Dawley rats (300-350 g; male)^[4]
Dosage:	0.30, 0.60, 0.90, 1.50, 1.75 μM
Administration:	Intrathecal injection; one time
Result:	Resulted the spinal block and displayed dose-dependent effect. Showed 100% blockades in motor function, proprioception, and nociception, with full recoveryduration of action about 41, 56, and 88 min, respectively, at 1.75 μM.

Molecular Weight

240.34

Formula

C₁₆H₂₀N₂

CAS No.

86-21-5

SMILES

CN(C)CCCC1=NC=CC=C1C2=CC=CC=C2

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

Handling Instructions (2659 KB)

References

[1]. Sharma A, et al. Classic histamine H1 receptor antagonists: a critical review of their metabolic and pharmacokinetic fate from a bird's eye view. Curr Drug Metab. 2003 Apr;4(2):105-29. [Content Brief]

[2]. Brown RD, et al. Alpha 1-adrenergic and H1-histamine receptor control of intracellular Ca2+ in a muscle cell line: the influence of prior agonist exposure on receptor responsiveness. Mol Pharmacol. 1986 Jun;29(6):531-9. [Content Brief]

[3]. Jangi SM, et al. Apoptosis of human T-cell acute lymphoblastic leukemia cells by diphenhydramine, an H1 histamine receptor antagonist. Oncol Res. 2004;14(7-8):363-72. [Content Brief]

[4]. Hung CH, et al. Spinal anesthesia with diphenhydramine and pheniramine in rats. Eur J Pharmacol. 2011 Dec 30;673(1-3):20-4. [Content Brief]

Pheniramine Related Classifications

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The molarity calculator equation

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

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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.

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