Rispenzepine (DF 594) is a muscarinic receptor antagonist. Rispenzepine has high affinity for intestinal muscarinic receptors, with preferential action at M1 and M3 receptor subtypes. This drug shows potent inhibitory effects on intestinal motility. In guinea pigs, rispenzepine significantly increases acetylcholine release in the trachea. A phase II study to test efficacy in asthma patients has been discontinued.

Sulisatin (also known as DAN-603) is an indolinone derivative patented by Andreu, Dr., S. A. as a laxative. In preclinical models, Sulisatin increases selectively the colon motility without modifying the speed of gastric, intestinal (small intestine) and caecal emptying in rats. Sulisatin is unable to inhibit water absorption in rat colon while small amounts of Sulisatin may inhibit it significantly.

Bunolol is non-selective beta-adrenoreceptor antagonist with significant antihypertensive, antiarrhythmic and local anesthetic activities. Bunolol is a racemic mixture and Levobunolol is greater than 60 times more potent than its dextro isomer in its beta-blocking activity. Bunolol is 3 times as potent as propranolol by i.v. administration in anesthetized dogs in antagonizing the cardiovascular actions of isoproterenol and the response to cardioaccelerans nerve stimulation. When oral doses were given to unanesthetized dogs with subsequent induction of anesthesia, Bunolol was 20 times as potent as propranolol. The β-adrenergic blocking activity of Bunolol appeared to be competitive, and the activity was largely restricted to the l-isomer. Bunolol is extensively metabolized by both oxidative and reductive routes.

KALAFUNGIN is an antimicrobial agent obtained from the culture broth of a soil isolate of Streptomyces tanashiensis, designated Streptomyces tanashiensis strain Kala UC-5063. It has in vitro activity against a variety of pathogenic fungi, yeasts, protozoa, and bacteria.

Dimoxamine is a memory adjuvant. Dimoxamine hydrochloride has been reported to facilitate the performance of naive rats in a massed trial shuttle box task. At doses that facilitated shuttle box responding, dimoxamine had no effect on unacclimated motor activity of rats nor on the rate of continuous avoidance responding by rats. Dimoxamine has a psychopharmacological profile that is different from other phenylalkylamines such as S-amphetamine and R-DOM. Dimoxamine may prove beneficial in the treatment of individuals having low or deteriorated levels of certain types of associative and psychomotor abilities. Dimoxamine substituted completely for LSD. Dimoxamine can be classified as a partial agonist of 5-HT receptors in sheep umbilical arteries.

Mazapertine (RWJ-37796) is an arylpiperazine antipsychotic with high affinity to dopamine D2 and D3, serotonin 5-HT1A and alpha 1A-adrenergic receptors. It was being studied in the treatment of schizophrenia.

Furosemide is a non-antibiotic bacterial urease inhibitor that can be used in the control of H. pylori-associated gastroduodenal disease.

Idrapril is an inhibitor of the angiotensin-converting enzyme the last is responsible for recurrent myocardial infarction in patients with left ventricular dysfunction. Idrapril participated in phase II clinical trials in essential hypertensive patients, where was shown that the drug was well tolerated. In addition, it was involved in preclinical studies as a potential drug to treat heart failure and postmyocardial infarction. However, the development of the drug was discontinued.

Hydromorphinol, an opioid, and is a derivative of morphine and possesses similar properties: sedation, analgesia, and respiratory depression. Hydromorphinol is under the control according to US Single Convention 1961.

Tazomeline (also known as LY 287041), a neuropsychiatric agent, is a muscarinic M1 acetylcholine receptor agonist that was studied in patients with cognitive dysfunction. Tazomeline participated in clinical trials for the treatment of Alzheimer’s disease and dementia. However, all these studied were discontinued for unknown reasons.