Companies
MedChemExpress LLC (MCE)
Products
MedChemExpress - Model Pheniramine ...

MedChemExpress - Model Pheniramine maleate -132-20-7

Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects[1][2][3][4].

Pheniramine maleate

MCE China：Pheniramine maleate

Brand：MedChemExpress (MCE)

Cat. No.HY-B0971

CAS：132-20-7

Synonyms：Prophenpyridamine maleate; Tripoton maleate; Pheniramine maleate

Purity：99.94%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

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

In Vitro：Pheniramine maleate inhibits CYP2D6, the specific P450-isozymes, to delay metabolic time and prolong antihistaminic effects[1]. Pheniramine maleate regulates cellular Ca2+ transmembrane action, and inhibits Ca2+ influx into BC3H-1 cells by inhibiting histamine with an IC50 value of 1.01 mM[2]. Pheniramine maleate (0.5, 1.0 mM; 24 h) induces cell apoptosis in human T-cell acute lymphoblastic leukemia cell lines[3]. Pheniramine maleate (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].

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

IC50 & Target：H1 Receptor 1.01 mM (IC50)

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]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。

MedChemExpress - Model Pheniramine maleate -132-20-7

MCE products for research use only. We do not sell...

Pheniramine maleate