A potent, selective and orally active receptor antagonist of leukotriene D4, verlukast (MK-571), was discovered and developed from a styrylquinoline lead structure based on a hypothetical model of the leukotriene D4 receptor. MK-571 blocks the action of LTD4 in animals and man, and is effective in a number of animal models of antigen-induced bronchoconstriction at plasma concentration at or below 2 ug/mL. MK-571 also blocks antigen-induced asthmatic responses in man. MK-571 is a potent and selective leukotriene D4 (LTD4) antagonist and ABCC multidrug resistance protein 1(MRP1) inhibitor. The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G-protein coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor. MK-571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. MK-571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors.

Clebopride is a dopamine antagonist drug. It is used to treat functional gastrointestinal disorder such as nausea or vomiting. Unchanged parent drug was the most abundant compound in human urine. Major metabolites included the hydroxylation at benzyl group to yield carbinolamine and its further N-dealkylation product, and the piperidine ring hydroxylation/oxidation metabolite (a lactam).

Potassium Glycerophosphate is a source of potassium. It is used in the treatment of nutritional deficiencies. Potassium supplements can be an important part of the recovery from or prevention of many different ailments and diseases. The most common of these include helping lower blood pressure and serving as a stroke preventative. Potassium can also be used to lower levels of calcium, to help with certain diseases including Alzheimer’s and Meniere’s. It may also help with some more common issues such as a common allergy, migraines, heavy acne, alcohol abuse, dizziness and confusion, extreme fatigue, recurring constipation, insomnia, anger and aggression, irregular heartbeat and stress. Potassium can either be taken as a supplement by mouth or it can be given intravenously to certain patients who require a faster dosing of the mineral or cannot take it orally.

Ritipenem (FCE 22101), a penem antibiotic, penicillin binding protein inhibitor, is potent against both gram-positive and -negative bacteria, and its acetoxymethyl ester (FCE 22891; ritipenem-acoxil) is orally available. Ritipenem is manufactured by Tanabe Seiyaku in the ritipenem acoxil prodrug form, which can be taken orally. It is not FDA approved in the United States.

Alifedrine, a beta-adrenergic partial agonist, significantly improved performance of the failing heart. Alifedrine resulted in a significant dose-dependent increase in cardiac output. There were significant reductions in peripheral resistance, but little observed change in arterial pressure. With intravenous alifedrine, there were significant increases in stroke volume with little change in heart rate. With the 40 mg oral dose, there was a small increase in heart rate There were no clinically or statistically significant changes in arterial (non-invasive), pulmonary artery, pulmonary capillary or right atrial pressures with any dose of alifedrine. No significant arrhythmias were noted clinically with the doses studied.

Sulfametrole is a sulfonamide antibiotic used typically in combination with trimethoprim. Sulfametrole combined with trimethoprim could provide a choice for difficult-to-treat infections, particularly when administered intravenously. Sulfametrole/trimethoprim is an alternative sulphonamide/trimethoprim combination available in several EU countries, including Austria and the Netherlands. Sulphonamide/trimethoprim combination is the most active antibacterial but sulfametrole and sulfametrole/trimethoprim did not overcome resistance to sulfamethoxazole and sulfamethoxazole/trimethoprim in Enterobacteriaceae.

Potassium Glycerophosphate is a source of potassium. It is used in the treatment of nutritional deficiencies. Potassium supplements can be an important part of the recovery from or prevention of many different ailments and diseases. The most common of these include helping lower blood pressure and serving as a stroke preventative. Potassium can also be used to lower levels of calcium, to help with certain diseases including Alzheimer’s and Meniere’s. It may also help with some more common issues such as a common allergy, migraines, heavy acne, alcohol abuse, dizziness and confusion, extreme fatigue, recurring constipation, insomnia, anger and aggression, irregular heartbeat and stress. Potassium can either be taken as a supplement by mouth or it can be given intravenously to certain patients who require a faster dosing of the mineral or cannot take it orally.

Sodium glycerol 2-phosphate (Disodium beta-glycerophosphate) is used for the preparation of thermo-sensitive chitosan hydrogen as a scaffold to construct tissue engineered injectable nucleus pulposus (NP). Since Sodium glycerol 2-phosphate (6 g/day) reduced the lithogenic index of bile in human subjects with cholesterol gallstones in a short-term study and facilitated dissolution of cholesterol gallstones in mice, Sodium glycerol 2-phosphate may have potential to help dissolve cholesterol gallstones in man. Sodium glycerol 2-phosphate is an alkaline phosphate inhibitor. Sodium β-glycerophosphate pentahydrate is used as a phosphatase inhibitor. It promotes bone matrix mineralization while delivering to osteoblasts by providing a source of phosphate ions. It is used in the development of hydrogels and scaffolds, which finds applications in tissue engineering and cell growth. It is used as an additive in isolation mediums by providing phosphate ions to isolate. It is utilized to promote mineralization in vitro by modulating bone cell metabolic activity.

Cefprozil, an oral cephalosporin antibiotic, is a mixture of antibiotic BMY-28100 (Z- or cis-isomer) and antibiotic BMY-28167 (E- or trans -isomer), the mixture having a Z- to E- isomer ratio in the range of 89:11 to 94:6. BMY-28167 (E- or trans -isomer) is less active when compared with BMY-28100 or isomeric mixture. There were no remarkable differences in the toxicity of the cis isomer, the trans isomer, or cefprozil (the isomeric mixture).

Pyridoxamine (PM) is one of three natural forms of vitamin B6. It is a critical transient intermediate in catalysis of transamination reactions by vitamin B6-dependent enzymes. In preclinical or clinical trials PM has demonstrated pharmacological potential for treatment of diabetic nephropathy, diabetic retinopathy, and hyperlipidemia, and for use in kidney stone preventive therapies. Although its precise mode of action in vivo is not yet clear, it is likely that at least three mechanisms are at play: inhibition of post-Amadori steps of the Maillard reaction; scavenging of reactive carbonyl compounds; and inhibition of toxic effects of ROS. Pyridoxamine was marketed as a dietary supplement, often as the hydrochloride salt, pyridoxamine dihydrochloride. However, in the United States, the FDA ruled in January 2009 that pyridoxamine must be regulated as a pharmaceutical drug because it is the active ingredient in Pyridorin, a drug designed to prevent the progression of diabetic nephropathy.