Sulopenem is a thiolanylthiopenem derivative patented by American multinational pharmaceutical corporation Pfizer Inc as an antibiotic with broad-spectrum antibacterial activity against most gram-positive and gram-negative bacteria. Sulopenem showed concentration-dependent bactericidal activities against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, and Acinetobacter calcoaceticus. Morphological observation using a phase-contrast microscope revealed that sulopenem induced spherical cell formation with E. coli and K. pneumoniae at lower concentrations and bacteriolysis at higher concentrations. Therapeutic efficacies of sulopenem against systemic infections in mice were almost equal to those of imipenem against Streptococcus pneumoniae.

FLEROBUTEROL is a beta-adrenoceptor agonist with potential antidepressant activity.

Tienoxolol is a benzoic acid derivative patented by Centre d'Activite et de Recherche Pharmaceutique Industrielle Biologique et Medicale as β-sympatholytic and diuretic. Tienoxolol acts as a beta-adrenergic receptor antagonist shows potent diuretic and natriuretic activity and, besides that anti-hypertension activity in preclinical models. In clinical trials, Tienoxolol significantly and dose-dependently reduced exercise-induced tachycardia. This effect started 1 h after drug administration, peaked between 4 h and 6 h and lasted at least 12 h.

Flusoxolol (Ro 31-1411), a pharmacologically active optical isomer of Ro 31-1118 is a cardioselective beta-adrenoceptor antagonist. Flusoxolol was studied for the treatment of patients with ischemic heart disorders; however, the further development of the drug has been discontinued.

Fomidacillin (also known as BRL 36650) is a type of penicillin with antibacterial activity. Studies on volunteers have shown that the drug possessed the bactericidal activity and could be a candidate for the treatment of gram-negative bacillary infections. However, information about the further development of this drug is not available.

AstraZeneca R&D Charnwood (formerly Astra Charnwood, a subsidiary of AstraZeneca) was developing sibenadet (Viozan, AR-C68397AA) for the potential treatment of chronic obstructive pulmonary disease and asthma. Sibenadet is a dual D2 dopamine receptor, beta2-adrenoceptor agonist that combines bronchodilator activity with the sensory afferent modulating effects associated with D2-receptor agonism. Development of sibenadet has been discontinued due to disappointing efficacy findings.

Nifenalol is the beta-receptor antagonist. It has optical isomers. The racemic mixture and the levo-isomer are active in antagonizing beta-receptors, but the dextro-isomer is inactive. The levo-isomer seems to be about twice as active in blocking beta-receptors as the racemate. Nifenalol is virtually devoid of local anesthetic properties in contrast to procaine, propranolol, and butidrine. Nifenalol exacerbated the fighting behavior in male mice by foot-shock. Nifenalol has been studied in patients with coronary artery disease. It afforded the coronary patient good protection against angina and ischemic changes in the EKG. It was further noted that nifenalol had no antiarrhythmic action and that it was devoid of evident side effects. Nifenalol possessed weak action against tremorine and oxotremorine induced tremor.

Pafenolol is a beta 1 selective adrenoceptor blocker that was studied in phase I clinical trial in Sweden for the treatment of arrhythmia. However, this study was discontinued.

Nardeterol (SOM-1122) was found to be a high-affinity, partial agonist for beta adrenergic receptors. SOM-1122 inhibited the binding of [125I]iodopindolol to membranes prepared from rat cerebral cortex and cerebellum. SOM-1122 bound to beta adrenergic receptors in vitro and in vivo, increased levels of cyclic AMP in slices of cerebral cortex in vitro and reduced the density of beta adrenergic receptors after chronic treatment. SOM-1122 also was found to be behaviorally active. It reduced locomotor activity and altered behavior maintained under DRL and multiple FlFR schedules. These behavioral effects of SOM-1122 are similar to those reported previously for other centrally acting beta adrenergic agonists.