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.

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.

ITROCINONIDE is a synthetic corticosteroid which showed no signs of systemic activity (cortisol depression).

Ciclactate is cyclohexanol derivative patented by N. V. Koninklijke Pharmaceutische Fabrieken Voorheen Brocades-Stheeman & Pharmacia as spasmolytics and blood vessel dilator. Ciclactate has never been marketed in the US and EU.

As a narcotic antagonist similar in action to naloxone, DIPRENORPHINE is used to remobilize animals after analgesia by super-potent opioid analgesics such as etorphine and carfentanil. It is not used in humans. Diprenorphine binds approximately equally to the three subtypes of opioid receptors (mu, delta, and kappa) and antagonizes them. This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene. The therapeutic efficacy of many other compounds can be decreased when used in combination with Diprenorphine (54 compounds mentioned on www.drugbank.ca).

Picoplatin is a sterically hindered platinum (II) complex with antineoplastic properties developed for the treatment of cis-platin-resistant cancer. Picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and transcription, and the induction of apoptosis. However, in Phase III trials, picoplatin failed to meet its primary endpoint for advanced cell lung cancer. It remains in development for other cancers.

Diamfenetide (aka diamphenethide) is a fasiolicide used in sheep. It is effective against immature flukes but with diminishing activity as the fluke ages. It has proven an effective compound for use in prophylactic programs against Fasciola hepatica. Diamphenethide is deacetylated in the host liver to an active monoamine and diamine. The amine of diamfenetide has an action which produces an elevation of malate concentration in Fasciola. Malate is an intermediary product of glucose in this parasite. It is known that dopamine, a putative neurotransmitter in Fasciola has a protective effect against diamfenetide but the mode of action of a diamfenetide has yet to be defined in greater detail.

Bitoscanate is a tasteless, odorless, colorless, needle-like crystalline solid material prepared from mustard powder acid and used as an anthelmintic against nematodes, especially hookworms (Necator sp.) and Ancylostoma duodenale. Side effects reported with therapeutic use have been nausea, vomiting, diarrhea, abdominal pain or discomfort, loss of appetite, dizziness or giddiness, vertigo, weakness, headache, and an itching sensation over the body. Such side effects have most often been mild and required no treatment. Bitoscanate is classified as an extremely hazardous substance in the United States as defined in Section 302 of the U.S. Emergency Planning and Community Right-to-Know Act (42 U.S.C. 11002), and is subject to strict reporting requirements by facilities which produce, store, or use it in significant quantities.

Mepiprazole is a psychotropic pyrazole derivative. Mepiprazole is a serotonin reuptake inhibitor and adrenolytic. In clinical studies, it demonstrated anxiolytic properties.

Detrothyronine is the (R)-(D)-form of triiodothyronine and has antihyperlipidaemic actions with beneficial effects upon coronary disease and hypertension. Detrothyronine has been tried in the treatment of hypercholesterolemia but its toxic effects outweigh any therapeutic advantage.