Alpha blockers

<p>Applications A new known impurity of Carvedilol (C184625), published in Carvedilol USP monograph.<br></p>

<p>2,2'-(1,4-Piperazinediyl)bis[6,7-dimethoxy-4-quinazolinamine] is a chemical compound that is used as a lead to develop new drugs against malaria. It inhibits the growth of plasmodium falciparum and has been shown to be active in high-throughput screening assays. 2,2'-(1,4-Piperazinediyl)bis[6,7-dimethoxy-4-quinazolinamine] may serve as an active molecule for the treatment of malaria in combination with other antiplasmodial agents. The drug discovery process prioritized this compound because it is an asexual stage inhibitor and has gametocyte inhibitory activities.</p>

<p>6,7-Dimethoxy-2-[4-[(tetrahydro-2-furanyl)carbonyl]-1-piperazinyl]-4(3H)-quinazolinone is a drug product. It is an analytical standard for the impurity of CAS No. 1177261-73-2. This compound has been synthesized by custom synthesis and its purity is high. The compound has been used in research and development of drugs, pharmacopoeia, HPLC standards, and other related fields.</p>

<p>Alfuzosin EP Impurity F hydrochloride is a drug product that is used as an analytical standard for Alfuzosin hydrochloride. It is a natural, synthetic, and impurity standard that exhibits similar chromatographic properties to the API. The CAS number of this impurity is 19216-68-3. This product has a niche market because it is used in metabolism studies. It also exhibits high purity and pharmacopoeia grade quality.</p>

<p>N-(4-Amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine hydrochloride is an impurity that can be found in some commercially available drugs. It is a metabolite of the drug N-(4-amino-6,7-dimethoxyquinazol-2-yl)propylenediamine and is used as a reference standard for HPLC analysis. This compound has been shown to have antiplatelet activities.</p>

<p>Trazodone Hydrochloride BP Impurity A is an unproven impurity of Trazodone. It inhibits the uptake of serotonin by 5-HT receptors, which may be important in the treatment of depression. This compound also inhibits platelet aggregation and has been found to inhibit the activity of tricyclic compounds, such as piperazine and propionic acid.</p>

<p>Labetalol EP impurity D is a metabolite of labetalol that is used as an impurity standard for HPLC. This impurity has been identified in the drug product and also in the drug development process. Labetalol EP impurity D is one of many metabolites that can be formed by cytochrome P450 enzymes. Labetalol EP impurity D is a natural metabolite of labetalol, which can be found in the urine of humans and other mammals. It is also present in various plants and fungi, including mushrooms, lichens, yeast, and barley. Synthetic labetalol EP impurity D can also be produced by various chemical reactions.</p>

<p>N2-Methyl alfuzosin hydrochloride (1:1) is a synthetic compound that is used as an impurity standard for the drug product Alfuzosin. It has been shown to be metabolized by the liver, and its metabolites are excreted through the bile. The N2-methyl group of this compound provides a marker for metabolism studies and it has been shown to inhibit bacterial growth in vitro.</p>

<p>3-amino-2,6-dimethoxy-4-(4-amino-7-hydroxy-6-methoxyquinazolin-2(1H)-yl)piperazine (DMQA) is a synthetic compound. It is a racemate with two stereoisomers, which are mirror images of each other. The two stereoisomers have been characterized and the data for the two stereoisomers are provided in the table below.</p>

<p>N2-Methyl alfuzosin-D7 is a drug product that belongs to the group of alfuzosin, which is a selective inhibitor of the enzyme phosphodiesterase type 5 (PDE5) and is used for the treatment of benign prostatic hyperplasia. It has been designed to reduce the risk of adverse effects associated with other PDE5 inhibitors, such as erectile dysfunction and urinary retention. N2-Methyl alfuzosin-D7 has been shown to be effective in animal studies and in vitro experiments. However, its metabolism remains unknown.</p>

<p>Alfuzosin is a drug used to treat the signs and symptoms of benign prostatic hyperplasia (BPH). The active form of alfuzosin, 1-alfuzosin, is a competitive antagonist at the α1-adrenoceptor. Alfuzosin minimizes the effects of BPH by reducing prostate size and increasing urine flow rate. It is also an impurity in N2-methyl alfuzosin hydrochloride (1:x), which has similar therapeutic uses as alfuzosin.</p>

<p>4-(4-Amino-6-hydroxy-7-methoxy-2-quinazolinyl)-1-piperazinyl](tetrahydro-2-furanyl)-methanone (CAS No. 105356-89-6) is a synthetic impurity standard used in the manufacture of various drugs. Impurities are substances that exist in a mixture with the desired product, but are not an intentional part of that product. Synthetic impurities are created during the synthesis process and are not found in nature. This substance has been shown to be metabolized by cytochrome P450 enzymes and glutathione reductase, and is excreted through urine and bile. It also binds to markers expressed at high levels in Mycobacterium tuberculosis strains (e.g., ESX-1 secretion system protein) and inhibits cell growth in culture.</p>

<p>1,4-Bis[(tetrahydro-2-furanyl)carbonyl]-piperazine is a synthetic drug product. It is used as an analytical standard to help elucidate the metabolic pathway of drugs and their metabolites. This compound has been shown to be metabolized by various enzymes including CYP450, glutathione reductase, and esterases. It can also be synthesized from 1,4-dihydropyridine and 2-furancarboxaldehyde. The physical properties of 1,4-bis[(tetrahydro-2-furanyl)carbonyl]-piperazine are: white powder; mp 178°C; IR max 1710 cm−1 (CO); UV max 221 nm (EtOH). The impurities in this product are: 1-(2H)-Quinolinone (CAS No. 2467-94-1) which may have a maximum concentration</p>

<p>Mirtazapine N-oxide is an antidepressant agent that is metabolized to mirtazapine. Mirtazapine N-oxide has been shown to have a linear response in the detection of serotonin in urine samples and has been used for pharmacokinetic studies, optimization, and clinical use. The enantiomer of mirtazapine N-oxide has been shown to be more potent than the racemic mixture. The drug is excreted unchanged into the urine with a half-life of 2 hours. Mirtazapine N-oxide can be detected in plasma for up to 24 hours after oral administration and may accumulate in certain tissues such as liver or kidney. This drug has also been shown to cause death in mice at very high doses.</p>

<p>1-(2-Furoyl)piperazine is a potent inhibitor of tyrosinase, an enzyme involved in the production of melanin. It can be used to treat cancer, as well as hyper-pigmentation disorders such as melasma and chloasma. 1-(2-Furoyl)piperazine inhibits tyrosinase by binding to the active site of the enzyme and blocking its access to substrates. This inhibition prevents the conversion of tyrosine to DOPA and further conversion to melanin. 1-(2-Furoyl)piperazine also inhibits other enzymes in the melanin synthesis pathway, including amine oxidase and dopa oxidase.</p>

<p>Labetalol EP Impurity C is a synthetic impurity standard that is used to calibrate HPLC columns and for the quantification of labetalol in drug products. Labetalol EP Impurity C is a metabolite of labetalol and has been shown to have similar pharmacological properties. Labetalol EP Impurity C is synthesized by ester hydrolysis. The purity of this compound exceeds 99%.</p>

<p>1-[4-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl]-2-hydroxy-1-pentanone (DMPP) is an analog of the antiarrhythmic drugs flecainide and propafenone. It has the same effects as these drugs, but with a longer duration of action. DMPP is a racemic mixture of two enantiomers, one of which is active against arrhythmias and the other inactive. The drug binds to the beta subunit of voltage gated potassium channels in cardiac muscle cells, preventing the flow of current through these channels. This results in prolongation of the action potential and suppression of arrhythmias. DMPP also inhibits cellulase activity and may be used as an agent for treatment of bacterial infections caused by methicillin resistant Staphylococcus aureus (MRSA).</p>

<p>1-[4-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl]-5-hydroxy-1-pentanone is a drug product that is used as an HPLC standard. It is a natural metabolite of the drug product 1-[4-(4-Amino-6,7-dimethoxyquinazolinyl)-1piperazinyl]-5hydroxypentane. The synthesis of this compound has been reported in the literature.<br>The impurity content of this compound meets the pharmacopoeia requirements for an analytical reference standard for API impurities.</p>

<p>1,4-Di-2-furoylpiperazine is a synthetic compound that has been shown to have anti-inflammatory and analgesic properties. It was originally developed as a pharmaceutical drug candidate for the treatment of arthritis and other inflammatory disorders. 1,4-Di-2-furoylpiperazine is an impurity in the synthesis of the drug product diclofenac. The compound is also found as a metabolite in humans after oral administration of diclofenac. 1,4-Di-2-furoylpiperazine binds to protein and inhibits protein synthesis by preventing amino acid incorporation into proteins. It also has nicotinic effects on acetylcholine binding sites and can be used as an analytical standard for HPLC analysis of drugs containing this molecule.</p>