Oxmetidine is an H2-receptor antagonist that was studied as a gastrointestinal agent. Oxmetidine possesses efficacy in the treatment of peptic ulcers. However, information about the further development of this drug is not available.

Ciclazindol is an indole derivative and monoamine uptake inhibitor patented by pharmaceutical company John Wyeth and Brother Ltd. as an antidepressant. Besides that, Ciclazindol is effective anorectic agent, inducing weight loss in rats and man. Ciclazindol was shown to inhibit ATP-sensitive K+ (K(ATP)) channel currents and stimulate insulin secretion from CRI-G1 insulin-secreting cells. The inhibition of KATP channel currents by ciclazindol is unaffected by the removal of intracellular Mg2+ ions and after trypsinization of the cytoplasmic surface of excised patches, treatments known to abolish sulphonylurea sensitivity.

Metoserpate (SU9064) is a sedative drug used in veterinary. PACITRAN (metoserpate hydrochloride) is indicated as a tranquilizer in stressed poultry.

Dimesone is a synthetic glucocorticoid with anti-inflammatory and anti-allergic activity.

Somantadine, an adamantane derivative, is an antiviral agent. Somantadine was synthesized by Pennwalt and has been undergoing tests for the treatment of herpes virus for nearly five years.

Oxilorphan (also known as levo-BC-2605) was developed as a long-acting, narcotic antagonist that has agonist properties. Oxilorphan is a partial agonist at the kappa-opioid receptor and antagonist of the mu-opioid receptor. During clinical trials, oxilorphan had led to dysphoria, which combined with its hallucinogenic effects, serves to limit its clinical usefulness. As a result, many patients who experienced these side effects refused to take additional doses in clinical trials.

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.

Indolapril (CI-907) is a new orally active prodrug of nonsulfhydryl angiotensin-converting enzyme (ACE) inhibitor, developed by Warner-Lambert/Parke-Davis Pharmaceutical Research for treating hypertension. Indolapril is epimer of trandolapril, well-known ACE inhibitor currently in the market for hypertension treatment. Indolapril (Monoester form) and it’s active component (diacid form) produced concentration related ACE inhibition in guinea-pig serum (IC50 for monoester -- 0.1 mkM and for diacid -- 2.6 nM). In isolated rabbit aortic rings and in rat and dog autonomic studies, Indolapril is highly specific in suppressing the contractile or pressor responses to angiotensin I. In two-kidney, one-clip Goldblatt hypertensive rats, single daily doses (0.03-30 mg/kg p.o.) produced dose-dependent decreases in blood pressure; 3 mg/kg lowered blood pressure to normotensive levels. In the spontaneously hypertensive rat, subacute administration of Indolapril produced the same decrease in blood pressure as that obtained in the renal hypertensive rat. In diuretic-pretreated renal hypertensive dogs, 10 mg/kg normalized blood pressure. For equivalent drops in blood pressure, heart rate increases were less in Indolapril than in enalapril-treated renal hypertensive dogs. No side effects were observed with CI-907 in any of the conscious animals. The antihypertensive response to Indolapril (0.03-1.0 mg/kg p.o.) was found to correlate with inhibition of vascular tissue ACE, but not plasma or brain ACE in two-kidney, one-clip renal hypertensive rats.

Quinpirole (LY 171,555) is a psychoactive drug and research chemical which acts as a selective D2 and D3 receptor agonist. Quinpirole is the most widely used D2 agonist in in vivo and in vitro studies. Specific quinpirole binding in rat brain was saturable, and dependent on temperature, membrane concentration, sodium concentration and guanine nucleotides. Saturation analysis revealed high affinity binding characteristics (KD = 2.3 nM) which were confirmed by association-dissociation kinetics. The regional distribution of [3H]quinpirole binding sites roughly paralleled the distribution of [3H]spiperone binding sites, with greatest densities present in the striatum, nucleus accumbens and olfactory tubercles. A variety of drugs, most notably monoamine oxidase inhibitors (MAOls), inhibit the binding of [3H]quinpirole, but not [3H]spiperone or [3H](-)N-n-Propylnorapomorphine, in rat striatal membranes by a mechanism that does not appear to involve the enzymatic activity of MAO. Clinically antidepressant MAOIs exhibited selectivity between sites labeled by [3H]quinpirole and [3H]spiperone as did a number of structurally related propargylamines and N-acylethylenediamine derivatives and other drugs such as debrisoquin and phenylbiguanide. Quinpirole has been shown to increase locomotion and sniffing behavior in mice and induces compulsive behavior symptomatic of obsessive compulsive disorder in rats.