130606-60-9

Usage

Uses

Used in Pharmaceutical Industry:
N-Desmethyldiltiazem, Hydrochloride is used as an active pharmaceutical ingredient for the development of antianginal and antihypertensive medications. Its role in regulating calcium release from intracellular stores in neutrophils makes it a valuable compound for treating conditions related to cardiovascular health.
Used in Research and Development:
In the field of research and development, N-Desmethyldiltiazem, Hydrochloride is used as a reference compound for studying the effects of Diltiazem on calcium regulation in neutrophils. This helps in understanding the underlying mechanisms of action and potential therapeutic applications of Diltiazem and its metabolites.
Used in Quality Control and Impurity Profiling:
N-Desmethyldiltiazem, Hydrochloride (Dilitiazem EP Impurity D) is used as a reference standard in the quality control and impurity profiling of Diltiazem pharmaceutical products. This ensures the safety, efficacy, and purity of the final drug product by monitoring the presence of impurities and their potential impact on the drug's performance.
Used in Drug Delivery Systems:
Similar to Gallotannin, N-Desmethyldiltiazem, Hydrochloride can also be employed in the development of novel drug delivery systems to enhance its bioavailability, delivery, and therapeutic outcomes. This may involve the use of various organic and metallic nanoparticles as carriers for improved drug targeting and reduced side effects.

Upstream product

• 42399-41-7 diltiazem 

Relevant academic research and scientific papers

Potent inhibition of human cytochrome P450 3A isoforms by cannabidiol: Role of phenolic hydroxyl groups in the resorcinol moiety

Aims: In this study, we examined the inhibitory effects of Δ9-tetrahydrocannabinol (Δ9-THC), cannabidiol (CBD), and cannabinol (CBN), the three major cannabinoids, on the activity of human cytochrome P450 (CYP) 3A enzymes. Furthermore, we investigated the kinetics and structural requirement for the inhibitory effect of CBD on the CYP3A activity. Main methods: Diltiazem N-demethylase activity of recombinant CYP3A4, CYP3A5, CYP3A7, and human liver microsomes (HLMs) in the presence of cannabinoids was determined. Key findings: Among the three major cannabinoids, CBD most potently inhibited CYP3A4 and CYP3A5 (IC50 = 11.7 and 1.65 μM, respectively). The IC50 values of Δ9-THC and CBN for CYP3A4 and CYP3A5 were higher than 35 μM. For CYP3A7, Δ9-THC, CBD, and CBN inhibited the activity to a similar extent (IC50 = 23-31 μM). CBD competitively inhibited the activity of CYP3A4, CYP3A5, and HLMs (Ki = 1.00, 0.195, and 6.14 μM, respectively). On the other hand, CBD inhibited the CYP3A7 activity in a mixed manner (Ki = 12.3 μM). Olivetol partially inhibited all the CYP3A isoforms tested, whereas d-limonene showed lack of inhibition. The lesser inhibitory effects of monomethyl and dimethyl ethers of CBD indicated that the ability of CYP3A inhibition by the cannabinoid attenuated with the number of methylation on the phenolic hydroxyl groups in the resorcinol moiety. Significance: This study indicated that CBD most potently inhibited catalytic activity of human CYP3A enzymes, especially CYP3A4 and CYP3A5. These results suggest that two phenolic hydroxyl groups in the resorcinol moiety of CBD may play an important role in the CYP3A inhibition.

Bacterial Biosynthetic P450 Enzyme PikCD50N: A Potential Biocatalyst for the Preparation of Human Drug Metabolites

Human drug metabolites (HDMs) are important chemicals widely used in drug-related studies. However, acquiring these enzyme-derived and regio-/stereo-selectively modified compounds through chemical approaches is complicated. PikC is a biosynthetic P450 enz