Aegeline is a compound extracted from Aegle marmelos (bael), a plant that has a long history of use in Ayurvedic medicine. Aegeline inhibited the histamine release from RBL-2H3 cells induced by DNP(24)-BSA. Aegeline showed strong inhibition when RBL-2H3 cells induced by Ca(2+) stimulants such as thapsigargin and ionomycin. Tthe inhibitory effects of aegeline on the histamine release from mast cells depended on the type of mast cell and also involved some mechanisms related to intracellular Ca(2+) signaling events via the same target of the action of thapsigargin or downstream process of intracellular Ca(2+) signaling in mast cells. Aegeline has shown antihyperglycemic as well as antidyslipidemic activities in the validated animal models of type 2 diabetes mellitus. Although some evidence from animal studies suggests that aegeline might lower blood sugar, this potential effect has never been studied in humans. This compound has been used as an ingredient in weight-loss aid products too, but again there is no evidence that it is effective for weight loss in humans. FDA recently issued an information update stating that FDA along with the Centers for Disease Control and Prevention are investigating more that 50 cases of liver damage. FDA also issued a warning letter to a company marketing a dietary supplement that contains aegeline, because it is not currently recognized as a legitimate ingredient for dietary supplements.

PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 uM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7. PF-4981517 is a very useful tool for understanding the relative roles of CYP3A4 versus CYP3A5 and the impact of CYP3A5 genetic polymorphism on a compound's pharmacokinetics.

trans-Ketoconazole was identified as impurity of an antifungal compound cis-ketoconazole. Cis-Ketoconazole displayed broad-spectrum in vivo activity in a wide range of experimental fungal infections caused by different fungi in a variety of animal models. trans-isomer of ketoconazole is less active than cis-ketoconazole.

Praziquantel, (+)- is the dextrorotated (+) isomer of Praziquantel. Praziquantel (PZQ) is the drug of choice against schistosomiasis. Since exposure of schistosomes to the drug is associated with calcium influx and muscular contraction, calcium channels have been suggested as the target. It is a specific pharmacological effect seen exclusively with the active levo-R(-)stereo isomer of the drug. Praziquantel, (+)- apparently contributes little to the therapeutic efficacy of Praziquantel. In vivo, single 400-mg/kg oral doses of Praziquantel, (-)- and Praziquantel, (+)- achieved worm burden reductions of 100 and 19%, respectively. Moreover, worms treated in vivo with Praziquantel, (+)- displayed an only transient hepatic shift and returned to the mesenteric veins within 24 h.

Pitavastatin lactone is the major metabolite of pitavastatin in humans. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase, which is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease. Uridine 5’ -diphosphate (UDP) glucuronosyl transferase (UGT) is critically involved in the lactonization of pitavastatin in man and animals. The metabolic and transporter profiles of pitavastatin in man are complex, involving acid/lactone interconversion. Both forms of pitavastatin are observed in-vivo following oral administration. Lactone form and pitavastatin differ in substrate activity towards uptake and efflux transporters.

Corydine is a naturally occurring compound which can be extracted from plants such as Chelidonium majus, Corydalis marschalliana, C. bulbosa, C slivenensis, Glaucium grandiflorum. Corydine has shown some efficacy as an anti-cancer compound in several cell models and was examined along with related compounds from Stephania dinklagei for antiprotozoal activities. (+)- and (-)- Corydine were tested as neuromuscular blocking agents were it was found that there was a modest preference for (+)-corydine.