Nuvenzepine is an mAChR antagonist previously in phase I clinical trials for the treatment of gastrospasm. Nuvenzepine substantially shares the antimuscarinic properties of pirenzepine but it is also endowed with a (weak) H1-blocking action. Nuvenzepine is selective for M1 receptors (pA2 = 6.63-7.74). Nuvenzepine, administered intraduodenally, displayed a long-lasting and dose-dependent inhibition of neostigmine-induced intestinal motility in anaesthetized cats. On ileal motor activity, the compound showed a potency 10 times greater than that of pirenzepine, and, although to a lesser extent, it was also active, unlike pirenzepine, on colonic stimulated motility. In conscious cats, nuvenzepine inhibited pentagastrin-stimulated gastric acid secretion resulting 25-30 times more potent than pirenzepine.

Imitrodast is thianaphthene derivative and thromboxane A2 inhibitor patented by Japanese pharmaceutical company Sankyo Co as antithrombotic agent.

Hoe 260 is a long-lasting and potent antisecretory and cytoprotective prostaglandin E2-analogue, having a favourable split between therapeutic gastric effects, effect on blood pressure and intestinal side effects. It is a prostanoid receptor agonist with antiulcerogenic activity.

Dimethylthiambutene is the synthetic narcotic analgesic agent. It has analgesic effect similar to those of meperidine. The (+)-enantiomer of dimethylthiambutene is more active than the (-)-isomer. Dimethylthiambutene clinically compared with meperidine (pethidine), but maintains the dependence-producing capability of morphine. It has had illicit use in Japan in the past. Dimethylthiambutene is under international control according to the UN Single Convention 1961 and its amendments, Schedule I.

Romazarit, (Ro 31-3948, 7), 2-[[2-(4-chlorophenyl)-4-methyl-5-oxazolyl]methoxy]-2-methylpropionic acid is a substituted heterocyclic alkoxypropionic acid. Romazarit was considered to be a potential disease-modifying antirheumatic drug. Romazarit was withdrawn due to its toxicity profile.

Norgesterone (norvinodrel, vinylestrenolone) is a progestin medication which was formerly used in birth control pills for women. The compound shows no androgenic and very little estrogenic activity; its progestational effect, as well as other properties, suggests its use as claudogenic agent. Norgesterone is an agonist of the progesterone receptor. It was used in combination with ethinylestradiol in birth control pills to prevent pregnancy.

Aceburic acid is the acetyl ester of gamma-hydroxybutyrate (GHB), it has analgesic effects as a prodrug to GHB. GHB is used medically as an anesthetic as well as a treatment for several neurologically affecting diseases.

Sanofi-Synthélabo has developed satavaptan (previously known as SR121463) as a non-peptidic vasopressin V2 receptor antagonist for the potential treatment for cardiovascular indications such as congestive heart failure (CHF) and hypertension. The drug reached phase II for these indications before the studies were discontinued. Satavaptan was also studied for the potential treatment of glaucoma. In addition, this drug was involved in phase III clinical trials in patients with ascites due to cirrhosis of the liver and in in patients with dilutional hyponatremia. However, the further development of the satavaptan was discontinued in 2009.

Esreboxetine (PNU-165442G) is the (S,S)-(+)-enantiomer of antidepressant reboxetine, a selective norepinephrine reuptake inhibitor. The (S,S)-enantiomer is a more potent inhibitor of norepinephrine transporter than (R,R)-enantiomer. Esreboxetine was being developed by Pfizer, primarily for the treatment of fibromyalgia.