Pexacerfont is a highly potent and selective CRF1 receptor antagonist that displays no agonist properties. It is specific for CRF1 receptors and has more than 1,000- fold less affinity for CRF2 receptors, and more than 100- fold less affinity for the CRF-binding protein. In extensive preclinical studies, pexacerfont has been shown to inhibit specific binding of CRF to rat, dog, monkey, and human CRF1 receptors. The functional anxiolytic effects of CRF1 receptor occupancy were demonstrated in two rodent models of anxiety, situational anxiety and elevated plus maze paradigms. Pexacerfont did not demonstrate efficacy compared to placebo for the treatment of generalized anxiety disorder in human. The bogus taste tests suggested some protective effect of pexacerfont against eating after a laboratory stressor. Pexacerfont had been in phase II clinical trials for the treatment of irritable bowel syndrome and depression depression.

Aventis developed safironil as a competitive inhibitor of collagen protein synthesis for the treatment of liver disorders. This compound participated in phase I clinical trial for the treatment of cirrhosis in Germany. In addition, it was studied for hepatic fibrosis treatment. However, information about the further development of this compound is not available.

m-Chlorophenylpiperazine (meta-chlorophenylpiperazine or mCPP) is a psychoactive substance, which is illegal in many countries but can be found on the black market. It induces endocrine, neurological and psychiatric effects. mCPP is a partial agonist at the 5-HT2C receptor but antagonized the 5-HT2B and 5-HT3 receptors. mCPP is also an active metabolite of the drug trazodone, which is used as an effective antidepressant drug with a broad therapeutic spectrum, including anxiolytic efficacy. It is known, that mCPP induces migraine attacks and that the decrease of food intake induced by the mCPP depends on its ability to act as a serotonin agonist is a brain.

Tazolol is a selective myocardial beta-blocking agent. Experiments on dogs have shown that this compound could be useful in patients with heart failure due to coronary artery disease. However, information about the current use of tazolol is not available.

Sulverapride is a methylsulfamoylbenzamide derivative patented by Societe d'Etudes Scientifiques et Industrielles de l'Ile-de-France for the treatment of lower urinary tract disorders

Sulrnazole (the former AR-L 115 BS) is a benzimidazole derivative with positive inotropic, positive chronotropic and vasodilator effects. Sulrnazole also has been shown to improve cardiac index and reduce pulmonary capillary wedge pressure without significant change in heart rate or arterial pressure. Intravenous administration caused a 217 per cent increase in cardiac output with a 25 per cent decrease in pulmonary wedge pressure. Short-term oral administration resulted in a 317 per cent increase in cardiac index and a 317 per cent increase in ejection fraction. Side effects have included visual blurring and transient colour blindness. Sulmazol has been demonstrated to improve regional wall motion in patients with ischemic heart disease and to abolish pacing-induced ischemia. Sulrnazole is an A1 adenosine receptor antagonist. It is also a phosphodiesterase inhibitor.

Spiramide (AMI-193) is a spiperone derivative, a selective 5-HT2A, (Ki = 2 nM) 5-HT1A (Ki = 50 nM), and D2 receptor (Ki = 3 nM) antagonist, with negligible affinity for the 5-HT2C receptor (Ki = 4300 nM). The ability of Spiramide to serve as a functional 5-HT2A antagonist in behavioral studies was demonstrated through studies in which Spiramide blocked the discriminative - stimulus effects of the 5HT2A agonist 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM).

Sorbinil (also known as CP-45,634), an aldose reductase inhibitor that has been in phase III clinical trials in preventing the development of diabetic retinopathy and neuropathy in persons with insulin-dependent diabetes. However, this research has been discontinued. It is also known, that sorbinil is oxidatively metabolized to a potentially toxic intermediate.

Linsitinib is an inhibitor of the insulin receptor and the insulin-like growth factor 1 receptor, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Linsitinib is in phase II clinical trials for the treatment of metastatic prostate carcinoma, gastrointestinal stromal tumors and other cancers. Common adverse events included fatigue, nausea hyperglycaemia and anorexia.