TZC-5665 (Oberadilol) is a pyridazinone derivative with vasodilatory and beta-adrenergic blocking activities and type III phosphodiesterase inhibitory action

Tipepidine (INN) also known as tipepidine hibenzate (JAN), is a synthetic, non-opioid antitussive and expectorant of the thiambutene class. The drug was discovered in the 1950s, and was developed in Japan in 1959. It is used as the hibenzate and citrate salts. The safety of tipepidine in children and adults has already been established. It is reported that tipepidine inhibits G-protein-coupled inwardly rectifying potassium (GIRK)-channel currents. The inhibition of GIRK channels by tipepidine is expected to modulate the level of monoamines in the brain. Tipepidine can improve attention deficit/hyperactivity disorder (ADHD) symptoms by modulating monoaminergic neurotransmission through the inhibition of GIRK channels. Tipepidine also is being investigated in depression, obsessive-compulsive disorder, and attention-deficit hyperactivity disorder (ADHD). As it acts on the central nervous system, overdose can cause altered mental status and other neurological symptoms; however, there have been few reports of tipepidine intoxication, including six cases in children and no cases in adults.

Tipepidine (INN) also known as tipepidine hibenzate (JAN), is a synthetic, non-opioid antitussive and expectorant of the thiambutene class. The drug was discovered in the 1950s, and was developed in Japan in 1959. It is used as the hibenzate and citrate salts. The safety of tipepidine in children and adults has already been established. It is reported that tipepidine inhibits G-protein-coupled inwardly rectifying potassium (GIRK)-channel currents. The inhibition of GIRK channels by tipepidine is expected to modulate the level of monoamines in the brain. Tipepidine can improve attention deficit/hyperactivity disorder (ADHD) symptoms by modulating monoaminergic neurotransmission through the inhibition of GIRK channels. Tipepidine also is being investigated in depression, obsessive-compulsive disorder, and attention-deficit hyperactivity disorder (ADHD). As it acts on the central nervous system, overdose can cause altered mental status and other neurological symptoms; however, there have been few reports of tipepidine intoxication, including six cases in children and no cases in adults.

Nepaprazole is a proton pump inhibitor of substituted 2-(2-pyridinylmethylsulfinyl)-1H-benzimidazole class evaluated as useful drug for the clinical treatment of peptic ulcer diseases. The effects of the TY-11345 (nepaprazole sodium salt) on gastric mucosal proton pump (H+/K(+)-ATPase) activity, gastric acid secretion and gastro-duodenal lesions were investigated in experimental animals. TY-11345 potently inhibited H+/K(+)-ATPase activity in isolated rabbit gastric mucosal microsomes and the inhibitory effect was enhanced under weak acid conditions. In Ghosh & Schild rats, intravenous injection of TY-11345 significantly inhibited gastric acid secretion stimulated by tetragastrin; the effect of TY-11345 was twice as potent as that of omeprazole. In pylorus ligated rats, TY-11345 inhibited basal gastric acid secretion by both the intraduodenal and oral routes with 9 and 5 times more greater potency than those of omeprazole, respectively. The antisecretory effect of TY-11345 persisted for more than 24 h in pylorus ligated rats. In experimental ulcer models, TY-11345 prevented the formation of water-immersion stress, ethanol or indomethacin-induced gastric lesions and mepirizole-induced duodenal lesions in rats. The antiulcer effects of TY-11345 were 3 to 15 times more potent than those of omeprazole. These results suggested that TY-11345 had potent antisecretory and antiulcer effects which are exerted by suppression of H+/K(+)-ATPase activity in gastric parietal cells. Nepaprazole sodium had been studied in phase II clinical trials for treatment of gastric ulser but this research has been discontinued.

YM-435 is a dopamine D1 agonist. The renal and cardiovascular effects of YM-435 may be suitable for the treatment of patients with renal insufficiency, heart failure and hypertension. It has been in phase II clinical trials for the treatment of heart failure and hypertension. YM435 may be useful in the preservation of renal function in ischemia-induced acute renal failure. Also, it might be a useful as therapeutic agent for the treatment of congestive heart failure.

Fabesetron is a dual 5HT3 and 5HT4 receptors antagonist that was developed in Japan for the treatment of chemotherapy-induced emesis and gastrointestinal disorders. The development of the drug was terminated in phase II.

YM-435 is a dopamine D1 agonist. The renal and cardiovascular effects of YM-435 may be suitable for the treatment of patients with renal insufficiency, heart failure and hypertension. It has been in phase II clinical trials for the treatment of heart failure and hypertension. YM435 may be useful in the preservation of renal function in ischemia-induced acute renal failure. Also, it might be a useful as therapeutic agent for the treatment of congestive heart failure.

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.

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.

Epirizole (also known as Mepirizole) is a nonsteroidal anti-inflammatory drug developed for the treatment of such conditions as chronic rheumatoid arthritis. Although the drug was tested in a clinical trial, its current status is unknown and is supposed to be discontinued. Epirizole is known to be a duodenal ulcerogen, and its effect is mediated by generation of ROS.