Cinpropazine is a coronary vasodilator drug. In the animal model of ischemia, the drug was found to attenuate myocardial acidosis.

Belarizine was studied as a cerebral vasodilator.

Rentiapril (SA-446) is an angiotensin-converting-enzyme (ACE) inhibitor that has antihypertensive activity. This compound binds to ACE and blocks the conversion of angtiotensin I to angtiontensin II. Angiotensin II has vasoconstrictive activity, which rentiapril prevents, leading to vasodilation. Rentiapril has been shown to inhibit ADE activity more strongly and for longer periods than two other ACE inhibitors (captopril, and alacepril), and reduces blood pressure more quickly and for a longer time in patients with renovascular hypertension. Because rentiapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, it increases sodium excretion and (subsequently) water outflow.

FEPRADINOL is an antiarrhythmic agent.

Ciprokinen is a renin inhibitor discovered by Roche. Ciprokinen inhibited human renin in a buffer and human plasma with an IC50 of 0.07 and 0.65 nmol/L, respectively. In animal models, acute and chronic administration of ciprokinen lead to a reduction in arterial blood pressure. Development of ciprokinen was discontinued at a preclinical stage.

Pomisartan, also known as BIBR-363, is an angiotensin type 1 receptor antagonist. It was investigated for the treatment of Congestive heart failure and hypertension. However, no development reports available at this moment.

Rotigaptide (previously known as ZP123) originally was developed by Zealand Pharma as a stable antiarrhythmic peptide analog, which maintains gap junction intercellular communication. Then this drug was licensed to Wyeth Pharmaceuticals where it studied in phase II clinical trials in patients with coronary artery disease and with atrial fibrillation. However, these researches have been discontinued.

Flupranone was invented as an antihypertensive agent that has never been marketed. Information about the current use of this drug is not available.

Tinabinol is a thiopyranobenzopyran derivative patented by Sharps Associates as tranquilizing agent. In preclinical modes Tinabinol shows good analgesic properties and causes ataxia in dogs at low doses.

Tolnapersine is an antihypertensive drug. It is a compound with mixed dopamine agonist and alpha-adrenoceptor antagonist activity. Tolnapersine at a dose of 50 mg resulted in a fall in mean blood pressure. Tolnapersine at the higher dose produced a significant tachycardia, which would be compatible with a compensatory response to vasodilation. Also, at the higher dose tolnapersine produces sedation. Many compounds have been reported as potential reversing agents of multidrug resistance. Tolnapersine yielded a good activity (ratio of > 10).