Alpha blockers

Leflunomide is a drug that belongs to the class of pyridones. It is used in the treatment of rheumatoid arthritis, juvenile idiopathic arthritis, psoriatic arthritis, and ankylosing spondylitis. Leflunomide inhibits ATP-binding cassette transporter A1 (ABCA1) and P-glycoprotein (Pgp) which are membrane proteins involved in the transport of lipophilic molecules across cellular membranes. Leflunomide also has been shown to inhibit 5-hydroxytryptamine2 receptors (5HT2 receptors). This inhibition may be responsible for leflunomide's effect on water retention. Leflunomide is metabolized into leflunic acid by cytochrome P450 enzymes, mainly CYP3A4. The activity of leflunic acid is similar to that of leflunomide.

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.

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.

Silodosin (KAD 3213) is an alpha-Adrenergic Blocker. The mechanism of action of silodosin is as an Adrenergic alpha-Antagonist.

Terazosin HCl (Hytrin) treats BPH and hypertension by blocking alpha1, affecting bladder and vessel muscles.

Applications A Labelled metabolite of Carvedilol which is a multiple-action, neurohormonal antagonist that is used in the treatment of hypertension. References Schaefer, W.H., et al.: Drug Metab. Dispos., 26, 958 (1998).

Terazosin: oral α1-blocker, relaxes blood vessels, treats BPH and hypertension.

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.

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.

Alfuzosin (SL 77499) is an alpha-1 adrenergic antagonist used to treat benign prostatic hypertrophy and urethral dysfunction.

Labetalol hydrochloride (Sch-15719W), a salicylamide derivative, is a non-cardioselective blocker of β-adrenergic receptors and α1-adrenergic receptors.

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.