Cronidipine (LF 2.0254) is a calcium channel blocker. LF 2.0254 inhibited in a time-dependent fashion K(+)- and Ca2(+)-induced contractions of rabbit aorta with respective IC50 of 2.7 nM and 1.7 nM. Cronidipine had a long-lasting antihypertensive action in spontaneously hypertensive rats and was able to decrease blood pressure and increase heart rate and plasma renin activity in hypertensive dogs.

Bremazocine, a kappa-opioid agonist has limited potential as a clinical analgesic, however, possesses a possible utility for the therapy of alcohol and drug addiction. It was shown that bremazocine-like drugs could lower intraocular pressure and to minimize ischemic damage, that could be used in the therapy of glaucoma and cardiovascular disease.

Indoxole is phenylindene derivative patented by Mead Johnson & Co. as antidepressants. Indoxole have potent activity in the prevention of reserpine-induced ptosis in mice.

Ampyzine is a pyrazine derivative patented by Warner-Lambert Pharmaceutical Co. as a central nervous system stimulant.

Anatibant was a selective small-molecule antagonist of the bradykinin B2 receptor that was undergoing clinical development with Xytis and Fournier for the treatment of brain injuries. Anatibant reduces brain oedema in animal TBI models. Noserious toxicity was found in Phase 1 clinical trials. Following subcutaneous administration of clinically relevant doses, there were no systemic effects but there was pain, inflammation and nodule formation at the injection site. Anatibant inhibits the binding of BK to the B2 receptor. After subcutaneous injection Anatibant is bio-available and crosses the BBB.

Carcainium is phenylcarbamoylmethyl derivative with local anesthetic and potent anti-tussive activity. In preclinical studies Carcainium significantly reduced the spontaneous and histamine-evoked discharges in Aδ-fibres originating from airway, rapidly adapting stretch receptors (RARs) without affecting histamine-evoked bronchoconstriction. Acute pre-treatment of guinea-pigs with aerosols of Carcainium prevent of capsaicin-evoked and citric acid-induced coughs.

Butopyrammonium is organic cationic compound.

Etorphine was the first potent opiate agonist employed primarily for use in non-domestic and wild species. Etorphine was 500 times as potent as morphine, with a very rapid onset and short duration of action. In morphine-dependent subjects, etorphine suppressed abstinence but for a shorter period than morphine. Etorphine is a full opiate agonist and binds to multiple opiate sites in the central nervous system. It is believed to produce its clinical effects through binding the µ-, δ-, and κ- opiate sites. It has a potent effect on depressing the respiratory centers of the CNS thus resulting in apnea being commonly seen in immobilized animals. Etorphine revolutionized the ability of biologists and veterinarians to safely capture and restrain many species that previously could not be handled. Etorphine is not currently commercially available due to lack of production by the manufacturer.

Fedotozine [(1R)-1-phenyl-1-[(3,4,5-trimethoxy) benzyloxymethyl]-N,N- dimethyl-n-propylamine, (2S,3S-tartrate], derived from the arylacetamide series, is an opioid drug which acts as a selective agonist for kappa(1a)-opioid receptor. Pharmacological studies have shown that fedotozine exerts a peripheral antinociceptive action, comparable with that of other kappa-agonists. Results of Phase III trials of fedotozine against irritable bowel syndrome and dyspepsia have ultimately been disappointing and was lack of efficacy in subsequent studies.

British Biotech was developing solimastat [BB 3644], an inhibitor of tumour necrosis factor and matrix metalloproteinase, as a potential treatment for colorectal cancer, inflammatory bowel diseases and rheumatoid arthritis. BB-3644 is an oral, broad-spectrum matrix metalloproteinase inhibitor (MMPI) structurally related to marimastat and BB-94. It is also >10-fold more active than marimastat in inhibiting the processing of cell-bound TNF-alpha. Solimastat development has been discontinued due to significant musculoskeletal toxicity.