Cynarine (Cynarin) is the most noteworthy active ingredient of the artichoke, and is considered a medicinal foodstuff due to its beneficial effect on the organism, derived from its condition as a stimulant of bile secretion (choleretic effect). Cynarine is present in artichoke leaves and has a beneficial effect on the control of gallstones, helps control cholesterol levels and improves gallbladder function. Chlorogenic acid and cynarin have been shown to have activity against oxidative stress in human leukocytes, whereas cynarin has also been shown to have hypocholesterolemic, hepatoprotective, and, more recently, antihuman immunodeficiency virus-1 (anti-HIV-1; 44) activities. Cynarin had marked antioxidant, anticholinergic, reducing ability, radical-scavenging, and metal-binding activities.

Acitemate is an antilipemic agent, cosidered to be HMG-CoA reductase inhibitor. It has been developed for the treatment of hyperlipidaemia, however development has been discontinued.

Zolenzepine, a nonselective antimuscarinic agent that was used as a reference compound.

Simfibrate, a derivative of clofibrate, is a hypolipidemic drug, that lowers serum chlolesterol and triglycerids. Under the brand name Cholesolvin it is indicated for hyperlipidaemia associated with arteriosclerosis, cerebral atherosclerosis, coronary arteriosclerosis, hypertension, diabetes.

Lidamidine, also known as WHR-1142A and Lidaral, is an alpha2-adrenergic receptor agonist that inhibits intestinal secretion, reduces intestinal transit, and inhibits smooth muscle contraction. Lidamidine hydrochloride is used to treat diarrhoea and other gastrointestinal disorders. Lidamidine’s intestinal antisecretory effects are mediated through the activation of peripheral alpha-2 adrenoceptors. Lidamidine crosses the blood brain barrier poorly and is therefore devoid of the centrally mediated alpha-2 effects that have limited the use of other alpha-2 adrenoceptor agonists in the intestinal tract.

Azacosterol (Ornitrol, 20,25-diazacholesterol dihydrochloride, SC 12937) is a cholesterol-lowering drug (hypocholesteremic) which was marketed previously but has since been discontinued. Azacosterol is a sterol derivative of cholesterol with two nitrogen atoms replacing two carbon atoms that acts as a hypocholesteremic agent by blocking delta-24-reductase. Azacosterol has the unintended side effect of causing myotonia. It is an avian contraceptive compound, which reduces fertility by inhibiting cholesterol synthesis. Azacosterol is also useful in the control of rodent populations.

Revaprazan (trade name Revanex) is a drug that reduces gastric acid secretion and is used for the treatment of gastritis and acid-related disease. It acts as an acid pump antagonist (potassium-competitive acid blocker) that reversibly inhibits H+, K+-ATPase by binding to the K+-binding site of the pump, thereby causing fewer side effects, compared with the irreversible proton pump inhibitors. Revaprazan is approved for use in Korea, but is not approved in Europe or the United States.

Niperotidine is an H2 antagonist structurally related to ranitidine. H2 antagonists inhibit gastric acid secretion by selectively blocking histamine receptor type 2. Niperotidine was proposed for the treatment of peptic ulcer. Bedtime dose of niperotidine inhibits nocturnal gastric acid secretion in healthy subjects. The duration of niperotidine action was 5 to 7 hours. Twenty-five cases of acute hepatitis (including one death from fulminant hepatitis) associated with niperotidine use were reported in Italy between March and August 1995 and drug was withdrawn from the market. The methylenedioxy group of niperotidine is known to undergo metabolism to catechol and quinone metabolites.

Xenalipin (4’-trifluoromethyl-2-biphenyl carboxylic acid) is a chemical compound which has been found to be an effective hypolipidemic agent in animal models. Significant reductions in serum cholesterol and triglycerides were observed in cholesterol-cholic acid-fed rats following oral doses of Xenalipin. Xenalipin was considerably more potent than clofibrate, nicotinic acid, and cholestyramine in the same model. Lipoprotein analysis showed that xenalipin reduced cholesterol and protein content in very low-density lipoprotein (VLDL), intermediate density lipoprotein (IDL), and low-density lipoprotein (LDL). Triglycerides were reduced in very low-density lipoprotein and intermediate density lipoprotein. Xenalipin was also effective in reducing serum cholesterol and triglyceride concentrations in normocholesterolemic rats. In diet-induced hypercholesterolemic African green monkeys, xenalipin reduced serum LDL-cholesterol concentrations. Xenalipin has a profile of activity which would be beneficial in therapy for hyperlipidemia.

Etofibrate is an ethylene glycol diester of clofibrate and nicotinic acid. The drug was used under the names Tricerol and Lipo-Merz, among the others, for the treatment of severe hypertriglyceridemia and mixed hyperlipidemia. The mechanism of etofibrate action implies activation of PPAR-alpha receptors.