Enoximone is an inhibitor of PDE3, which is used for the treatment of congestive heart failure. Also enoximone was shown to inhibit PDH in cardiac myocytes. The inhibition was shown to occur secondary to stimulating fatty acid oxidation

Betamipron (BP) is an amino acid derivative that has benzoyl and carboxyl groups in its structure, and it also has very low toxicity in mammals (LD50 in the rat, more than 3,000 mg/kg, i.v.). BP is a renal anionic transport inhibitor and decreases nephrotoxicity caused by high doses of carbapenems, anionic drugs, by inhibiting the drug accumulation in the renal cortex. BP significantly inhibited organic anion uptake by human organic anion transporter 1 (human-OAT1) and human-OAT3 in a dose-dependent manner. Panipenem-betamipron is marketed as Carbenin® (Sankyo Company, Tokyo, Japan).

Methyllycaconitine is a diterpenoid alkaloid found in many species of Delphinium (larkspurs). Methyllycaconitine is a potent antagonist for α7-containing neuronal nicotinic receptors. Methyllycaconitine (as mellictin) is used in some countries as a myorelaxant for treatment of pyramidal and extrapyramidal motoric disorders, such as pyramidal insufficiency, Parkinson disease, meningocephalitis and other disorders.

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.

Calmatel contains piketoprofen and belongs to the group of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). This medicine is indicated in adolescents over 12 years and adults for local pain relief and mild and occasional inflammation caused by: small contusions, bruises, strains; torticollis or other contractures; lumbago; minor sprains caused because of a twist.

Avizafone is a water-soluble peptide prodrug of diazepam that is hydrolyzed by an aminopeptidase to liberate lysine and diazepam Avizafone was developed by the French military to terminate seizures caused by battlefield nerve agents. Diazepam has a faster entry to the general circulation and achieved higher maximum concentration after injection of prodrug than after the parent drug and this is extremely valuable in nerve agents poisoning conditions.

Endralazine (6-benzoyl-3-hydrazino-5,6,7,8-tetrahydropyrido-(4,3-c)-pyridazine mesylate) is a peripheral vasodilator drug, which acts by direct relaxation of the smooth muscle fibres of the peripheral arterial vessels. Endralazine has been used as an antihypertensive agent.

Tiaprofenic acid is a non-steroidal, anti-inflammatory, analgesic compound, which nonselectively inhibits cyclooxygenase protein. Tiaprofenic acid was approved in Europe for the symptomatic relief of arthritis, ankylosing spondylitis and other inflammatory-rheumatic disorders as well as the painful conditions after injury.