Bitopertin is a Glycine transporter type 1 inhibitor which was developed by Hoffmann-La Roche for the treatment of patients with schizophrenia. The drug was shown to be potent in vitro, however it failed to meet primary endpoints in phase III. Bitopertin was also tested for the treatment of obsessive-compulsive disorder, but the development stopped in phase II.

Sulfinalol is a hydroxyphenylalkanolamine derivative patented by Sterling Drug Inc. as the antiarrhythmic, antihypertensive, vasodilating, and adrenergic agent. Oral administration of sulfinalol reduces the pressure of conscious spontaneously hypertensive rats. Antihypertensive action of sulfinalol was inhibited by propranolol pretreatment. Sulfinalol demonstrates effective beta-adrenergic blockade at the antihypertensive dose tested as judged by inhibition of the chronotropic responses to sympathetic stimulation and isoproterenol in pithed rats. In the renal hypertensive dog. sulfinalol lowered both systolic and diastolic blood pressure to normal values with an only slight change in heart rate.

CS-834 is a beta-lactam antibiotic of a carbapenem class, developed by the Japanese company Sankyo Co. Ltd. CS-834 is an ester-type prodrug of the active metabolite R-95867. The drug showed potent and well balanced antibacterial activity as well as stability against dehydropeptidase-I. The in vivo efficacy of CS-834 was evaluated in murine systemic infections caused by 16 strains of gram-positive and -negative pathogens. The efficacy of CS-834 was in many cases superior to those of cefteram pivoxil, cefpodoxime proxetil, cefdinir, and cefditoren pivoxil, especially against infections caused by S. aureus, penicillin-resistant S. pneumoniae, E. coli, Citrobacter freundii, and Proteus vulgaris. Pharmacokinetics of CS-834 was evaluated in healthy male volunteers, but no further clinical development of the drug was reported.

Cefmepidium is a semisynthetic cephalosporin with broad antibacterial activity against penicillin-resistant strains.

Razupenem (also known as PZ-601 or PTZ601) is an anti-MRSA carbapenem antibiotic. It is active against Enterobacteriaceae and Gram-positive bacteria including methicillin-resistant staphylococci and enterococci, and was investigated as potential alternative drug (replacing common antibiotics) against resistant bacteria. In healthy male volunteers, razupenem did not cause serious adverse events. The potential effect and safety of razupenem has been evaluated in a phase II clinical trial studying skin infection.

Idropranolol is a beta–adrenoceptor blocking agent that has never been marketed.

Mantabegron is an adamantane derivative with β3-adrenoreceptor agonist activity.

Zoleprodolol was developed as an adrenoreceptor antagonist. Information about the current use of this compound is not available.