Tiprenolol (DU21445) has been shown by both in vitro and in vivo animal experiments, to possess strong beta-adrenergic blocking but a relatively less strong negative inotropic activity. The same report also demonstrated by its inhibiting influence on spontaneous mobility of rat uterus, an intrinsic beta-sympathomimetic activity. Tiprenolol reveals effects similar to propranolol. Tiprenolol was shown to have significantly less heart rate slowing effect at rest than propranolol. However, all other measurements failed to show any difference of statistical significance between the two drugs with respect to any negative inotropic or beta‐blocking activity. The administration of tiprenolol or propranolol depressed the arterial pressure and caused the deaths of some dogs in which a coronary artery had been ligated.

Tigemonam is a dialkylazetidinone derivative patented by E. R. Squibb and Sons, Inc. as a beta-lactam agent useful for the treatment of bacterial infections. Of the orally active beta-lactams, tigemonam is one of the most potent, with a spectrum of activity similar to that of aztreonam and highly resistant to hydrolysis by the beta-lactamase enzymes. Tigemonam inhibits 90% of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis tested. In localized infections, tigemonam also demonstrated excellent in vivo activity. In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., tigemonam was very effective. In a rat lung model with Klebsiella pneumoniae, tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin.

Cefetecol is a broad-spectrum cephemcarboxylate derivative with antibacterial activity patented by British pharmaceutical company Glaxo Group Ltd.

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.