Aclatonium (also known as aclatonium napadisilate) is a cholinergic agonist that has been developed and used in Asia as an activator of gastrointestinal motility.

Linsidomine (SIN-1, chemically 3-morpholinosydnonimin), is a vasodilator and antianginal drug. It is the direct hepatic metabolite of molsidomine. The dosage recommended by its manufacturer for its initial purpose, coronary angiography, is 0.4-1 mg. Contrary to molsidomine, which is widely used as an antianginal drug, linsidomine is used only for coronary angiography. The plasma half-life of Linsidomine is about 1 hour. Linsidomine is nonenzymatically metabolized to SIN-1A which spontaneously releases NO. NO, probably released directly from nonadrenergic, noncholinergic (NANC) nerves in the penis, is believed to cause smooth muscle relaxation by stimulating the soluble form of guanylate cyclase leading to an increase of intracellular cyclic guanosine 3',5' monophosphate (cGMP) with subsequent smooth muscle relaxation. Linsidomine also hyperpolarizes the cell membrane, making the smooth muscle less susceptible to adrenergic stimulation. NO further interacts with platelets when released intraluminally causing an increase in cGMP that decreases platelet aggregation and adhesion

Bopindolol (4-[benzoyloxy-3-tertbutylaminopropoxy]-2-methylindole hydrogen malonate) is an indole beta-adrenoceptor antagonist bearing a benzoyl ester residue on the beta-carbon atom of the propanolamine side chain. Bopindolol is metabolized by esterase to benzoic acid and an active metabolite, 18-502 [4-(3-t-butylamino-2-hydroxypropoxy)-2-methyl indole], which is further metabolized to 20-785 [4-(3-t-butylaminopropoxy)-2-carboxyl indole]. Bopindolol produces sustained blockade of beta 1- and beta 2-adrenoceptors, has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is used in the treatment of hypertension. In limited trials bopindolol has also successfully reduced symptoms in patients with angina pectoris, anxiety and essential tremor.

Tiaramide is an anti-inflammatory and analgesic drug, which was developed by Fujisawa Pharmaceutical (now Astellas pharma) and used in Japan under the name Solantol for the treatment of different pain and inflammatory disorders. Later on, Astellas recalled the product by reasons other than safety. The mechanism of tiaramide action is unknown.

Dextromoramide is a synthetic strong-acting opioid and full mu-opioid receptor agonist. Dextromoramide is a Schedule I drug illegal to possess. The current indication for Palfium® (dextromoramide) is severe acute or chronic pain requiring opioids, such as post-operative pain, and pain associated with bone fractures, malignancies and acute renal/biliary colic attacks in adults.

Fendiline or Sensit (N-(3,3-diphenylpropyl)-(1-phenylethyl)-amine), is a diphenylalkylamine blocker of L-type calcium channels. Fendiline is an anti-anginal agent for the treatment of coronary heart disease. Pharmaco-dynamically, it exerts the typical calcium as well as calmodulin antagonistic actions: inhibition of the transmembrane calcium current, smooth muscle relaxation, negative inotropism, cardioprotection, inhibition of calmodulin-activated myosin light-chain kinase and phosphodiesterase. Pharmacokinetics reveal slow onset of action and a long half-life. The anti-anginal and anti-ischaemic efficacy of fendiline has been proven in several placebo-controlled, double-blind trials. Fendiline is an FDA-approved, albeit now clinically obsolete. Additionally, fendiline is a specific inhibitor of K-Ras plasma membrane localization that also inhibits K-Ras signal output and blocks the proliferation of K-Ras-transformed tumor cells.

Fenbutrazate is a prodrug of phenmetrazine, a psychostimulant for the treatment of obesity. Fenbutrazate acts as an agonist of monoamine transportes upon conversion to the active metabolite. The drug is no longer marketed due to its addictive profile.

Indisetron dihydrochloride (N-3389) was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 29, 2004. It was co-developed and co-marketed as Sinseron by Kyorin & Yakult Honsha in Japan. Indisetron is a dual serotonin 5-HT3 and 5-HT4 receptor antagonist. It is indicated for the treatment of prophylaxis of chemotherapy-induced nausea and vomiting, it’s administered once daily. Indisetron is metabolized in the liver, and CYP1A1, CYP2C9, CYP2D6, and CYP3A4 are involved in its metabolism. However, indisetron is unlikely to cause drug interactions at clinical doses because the effective plasma concentrations are lower than those necessary for inhibiting the metabolic enzymes. No drug interaction has been reported. Indisetron antagonizes 5-HT4 receptors, as well as 5-HT3 receptors, and this characteristic is expected to contribute to its clinical efficacy.

Indanazoline, an imidazoline derivative, (E-VA-16, as monohydrochloride active substance of Farial) is a nasal decongestant. As a nasal spray it can be used for the treatment of acute, chronic and allergic rhinitis. It is characterized by a pronounced vasoconstrictive action after local or intravenous application. This is due to a direct action of the compound on alpha-adrenergic receptors. When applied systemically Indanazoline being a peripherally acting alpha-sympathomimetic induces a rise in blood pressure and a reduction of heart rate and exerts antiphlogistic, spasmolytic, hyperglycemic and diuretic actions. When given by the intranasal route the substance influences blood pressure and heart rate only at concentrations considerably higher than those intended for use in therapy. After enteral administration the effective doses also markedly exceed the single therapeutic doses. There was no evidence of side-effects restricting the use of the drug as compared to other imidazoline derivatives.

Histapyrrodine was investigated as a neuro-sedative drug for the treatment of anxiety and states of aggression.