Vinburnine is a nutritional product, a peripheral vasodilator with cerebral activities that also act as a cerebral metabolic stimulant and appears to be able to relax the smooth muscle cells within the walls of blood vessels. (+/-)-Eburnamonine is the racemate of the alkaloid Vinburnine. Dextrorotatory, levorotatory, and racemic forms of eburnamonine exist in nature. The (-)-form, also known as vincamone (isolated from Vinca minor), is a drug that possesses a stimulating activity for muscle and is used as cerebrotonic, whereas both enantiomers have hypotensive effects.

Difemerine is antimuscarinic agent. It is used in the symptomatic treatment of visceral spasms. It may have anticholinergic side effects like dry mouth, dizziness, blurred vision and drowsiness. Anticholinergics must be used with caution in glaucoma and prostate hypertrophy patients.

Alaproclate is a selective 5-HT uptake inhibitor. Alaproclate enantiomers block potassium and NMDA receptor currents in a stereoselective manner. Alaproclate was practically devoid of action on a number of receptors as examined in binding studies in vitro: 5-HT, histamine-H1, alpha 1, -alpha 2-adrenergic and dopamine D2 receptors. Alaproclate was investigated in trials for the treatment of depression and dementia.

TILIDINE is a low to medium potency opioid analgesic. It is metabolized to its active metabolites, nortilidine and bisnortilidine. Its analgesic activity is largely exerted through nortilidine which is a potent agonist at Mu opioid receptors.

Amphecloral (INN: amfecloral) is a phenethylamine derivative which was patented in 1960 as an amphetamine pro-drug with prolonged duration of action. Amfecloral was used as an appetite suppressant under the trade name Acutran, but is now no longer marketed. It is an anorectic drug with little to no stimulant activity. Amphecloral is metabolized to both d-(S)- and l-(R)-amphetamine.

Tiracizine a drug belongs to the new class I antiarrhythmic agent was studied in patients with ischemic heart disease, where was shown, that the drug could decrease myocardial contractile function.

Suloctidil is considered to be calcium antagonist. In addition to its vascular antispasmodic activity, suloctidil affects blood platelets and enhances brain energy metabolism. Suloctidil was being evaluated in many clinical trials for use in dementia and thrombotic disorders. Suloctidil induces hepatotoxicity.

Terodiline is a racemic compound, and its main indication was detrusor instability syndrome. With effects on detrusor muscles, terodiline was used for bladder incontinence. Terodiline has both anticholinergic and calcium antagonist properties and, as a result, effectively reduces abnormal bladder contractions caused by detrusor instability. When administered to adult patients with urge incontinence (generally as a 25mg twice-daily dose) terodiline reduces diurnal and nocturnal micturition frequency and incontinence episodes. The (R)-enantiomer of terodiline (R( )-terodiline) can trigger cardiovascular toxicities, such as LQTS and TdP, which led to its withdrawal in 1991. Terodiline under the brand name Micturin was licensed and marketed in the United Kingdom, in 1986, for the management of a specific form of urinary incontinence, detrusor instability. It was eventually marketed in 20 other countries, mainly in Europe and Japan, but not the United States of America.

Otilonium is a musculotropic spasmolytic agent belonging to the family of quaternary ammonium derivatives and successfully used in the treatment of patients affected by Irritable bowel syndrome (IBS) due to its specific pharmacokinetic and pharmacodynamic properties. The positive polarity of the head of the Otilonium molecule determines the main pharmacokinetic property of this drug: a minimal systemic absorption and the consequently high safety profile. Studies on animal models revealed a specific Otilonium accumulation in colonic circular muscle at therapeutic µm concentrations, while its plasma levels were 1000 times lower, together with a poor penetration of the drug in the central nervous system. Consistently, after oral administration to healthy volunteers, the Otilonium plasmatic concentration was very low, less than 1% of the drug was eliminated by urine, and 97% was eliminated by feces. Recent clinical studies showed comparable safety and tolerability for Otilonium and placebo. Otilonium was shown to inhibit the main patterns of human sigmoid motility in vitro, including: the tone of smooth muscle cells (SMCs); the rhythmic phasic contractions induced by the interstitial cells of Cajal; and the strong contractions induced by stimulation of enteric motor neurons mainly by blocking the calcium influx through L-type calcium channels on SMCs. Recent in vitro studies using cultured human colonic SMCs to further assess the musculotropic spasmolytic properties of Otilonium confirmed that this drug causes smooth muscle relaxation through the inhibition of voltage-gated calcium channels (L-type > T-type) and the inhibition of muscarinic and tachykinergic effects.

Zofenopril is an inhibitor of Angiotensin Converting Enzyme (ACE), which is approved in Europe for the treatment of hypertension and acute myocardial infarction.