Clomifenoxide (clomifene N-oxide) is a metabolite of clomifene, a nonsteroidal ovulatory stimulant, which is used clinically for the treatment of ovulatory dysfunction in women desiring pregnancy. Compared to clomifene, clomifenoxide exhibits weaker binding to estradiol receptors.

Dilopetine is a racemic mixture of (+)-E-6006 citrate (E-6101) and (-)-E6006 citrate (E-6102) enantiomers being developed as a potential antidepressant. Initial experiments indicate that dilopetine exhibits an antidepressant profile in tests with mice and rats. Dilopetine has been observed to normalize the increased substance P levels in the periaqueductal gray of rats during stressor exposure (Hamon, personal communication), suggesting that the drug may function by inhibiting substance P release. Treatment with dilopetine reduced the vocalizing of isolated guinea pig pups in a dose-dependent fashion.

Aprikalim [RP 52891, RPG 52891] is a potent, specific, and selective opener of ATP-sensitive K+ (KATP) channels. By virtue of this pharmacological property, aprikalim affords cardioprotection in experimental models of ischemia/reperfusion injury, and, at higher doses, also causes peripheral or coronary vasodilatation. It is undergoing phase II clinical trials with Aventis Pharma for the treatment of asthma; heart failure; hypertension; myocardial ischaemia.

Methyldihydromorphine is a synthetic narcotic analgesic related to the morphine. This compound has no pharmaceutical value in the US.

Fluotracen (SKF-28,175) is a tricyclic drug which possesses dual antidepressant and antipsychotic activity mediated through blockage of GABA(A) receptors.

Solpecainol [EGIS 2936, EGYT 2936] is a sodium channel antagonist with antianginal and class I antiarrhythmic effects. It was in phase II clinical trials with Egis Pharmaceuticals for the treatment of angina pectoris and arrhythmias, but this development was discontinued.

Nemazoline (A-57219) is a nasal decongestant. It has alpha 1-agonist/alpha 2-antagonist activity and was more effective and long-acting than oxymetazoline on canine nasal mucosa, in-vitro and in-vivo. Upon intranasal administration to dogs, the compound was devoid of systemic effects up to a concentration 1000 times that needed for local decongestant effect (1.65 micrograms, atomized from a 1 microgram mL-1 solution) suggesting limited mucosal absorption. After nasal administration to rats for 15 days at a concentration 1000 times greater than that required for nasal decongestion, no mucosal tissue toxicity or systemic effects were seen.

Guaietolin was used as an oral expectorant.