Perfomedil is a vasodilator. Perfomedil is a buflomedil analog. Perfomedil like its parent compound buflomedil, antagonizes both alpha1- and alpha2-adrenoceptors. An important difference between perfomedil and its parent compound is the preferential antagonism exerted against alpha2-adrenoceptors. In the saphenous vein of the dog perfomedil acts as a relatively weak alpha-adrenergic blocker in vascular smooth muscle, with a preferential effect on postjunctional alpha2-adrenoceptors. At the adrenergic nerves, the compounds inhibit prejunctional alpha2-adrenoceptors and displace stored transmitter.

Vebufloxacin (OPC-7241) is a nalidixic acid analog. It exhibited potent antibacterial activity against gram-positive and -negative bacteria, including Staphylococcus aureus and Pseudomonas aeruginosa.

Amsilarotene (TAC-101) is a retinobenzoic acid (RAR) derivative with high affinity to the RAR-alpha receptor. It is a Retinoic acid receptor alpha antagonist. Amsilarotene is an orally absorbed synthetic retinoid. This analogue of vitamin A (retinol) binds to nuclear retinoic acid receptor-a (RAR-a), activates RAR-a transcriptional activity, and has shown antitumor activity in primary and metastatic preclinical models of liver cancer. Amsilarotene inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting in cell cycle arrest. This agent also causes a cytotoxic decline in cyclin A and thymidylate synthase expression.Amsilarotene inhibits tumor growth in the liver with low toxicity and markedly improves survival in both primary HCC and metastatic colon cancer models. It was in phase II clinical development with Taiho Pharmaceutical for liver cancer, however it was discontinued.

Diproleandomycin is a semisynthetic antibacterial agent. This antibiotic produced by Streptomyces antibiotocus.

Flutiazin was studied as an anti-inflammatory agent to use in veterinary. Information about the current use of this agent is not available.

Venritidine [D 16637] is an H2-antagonist which appears to undergo phase I clinical trials in the United Kingdom and preclinical investigation in Germany as a gastric ulcer treatment.

Lusaperidone (R107474) is a potent and relatively selective alpha(2)-adrenoceptor antagonist. It was under clinical evaluation for the treatment of depression, characterized by anergia and lack of drive. However, further clinical development has been stopped. Radiolabeled lusaperidone may be used as a potential radioligand for studying alpha(2)-adrenoceptors using PET.

Hoquizil, a phosphodiesterase inhibitor, was used as a bronchodilator agent. Information about the current use of this drug is not available.