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).

Palosuran, also known as ACT-058362, a potent and specific antagonist of the human UT receptor. Urotensin inhibition with palosuran was a promising alternative in pulmonary arterial hypertension. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Palosuran improves pancreatic and renal function in diabetic rats. Phase-II clinical trials for diabetic nephropathies and cardiovascular disorders were discontinued.

Pipratecol is substituted thienoimidazole. It is the H+/K(+)-ATPase inhibitor. In a high concentration of 10(-4) g/ml, pipratecol increased the amplitude of isolated guinea-pig atrial contractions while decreased the rate. But, in a low concentration of 10(-8) g/ml, the drug decrease the amplitude and increased the rate slightly. The effects of adrenaline and noradrenaline were suppressed by the preceding addition of pipratecol, while that of isoproterenol was scarcely. The effect of pipratecol on atrial contractions was hardly influenced by reserpine with which the animal had been pretreated 24 hours before the sacrifice of animal. The augmentative effect of nicotine on atrial contractions was slightly suppressed by the preceding addition of pipratecol. From these results, it was assumed that pipratecol has some affinity with the adrenergic receptor of atria. As a peripheral vasodilator it has been used in conjunction with raubasine in the treatment of cerebrovascular disorders. Pipratecol was used as antiulcerative agent also.

Abitesartan is an angiotensin II receptor antagonist, antihypertensive (non-peptidic) agent.

Mazokalim is a potassium channel agonist. It was studied in the treatment of asthma and hypertension.

Ataciguat is a novel anthranilic acid derivative that belongs to a new structural class of sGC activators which are capable of activating the oxidized form of sGC. Ataciguat, a nitric oxide-independent soluble guanylate cyclase activator, is being developed by Sanofi (previously sanofi-aventis), in collaboration with Mayo Clinic and National Center for Advancing Translational Sciences. Ataciguat is in phase II clinical trials for the treatment of aortic valve stenosis. It had been used to treat neuropathic pain and peripheral arterial disease, but this research has been discontinued.

Naminidil, a potassium channel opener, was under development with Bristol-Myers Squibb as a topical treatment for androgenetic alopecia. The research has been discontinued.

Trixolane is a spasmolytic, vasodilator, choleretic agent.

Ralinepag is a cyclohexyl amide derivative patented by Arena Pharmaceuticals, Inc. as agonists of the human prostacyclin (PGI2) receptor useful for the treatment of pulmonary arterial hypertension. Ralinepag shows selectivity in both binding and functional assays with respect to most members of the prostanoid receptor family and a more modest 30-50-fold selectivity over the EP3 receptor. Ralinepag had an excellent PK profile across species. Enterohepatic recirculation most probably contributes to a concentration-time profile after oral administration in the cynomolgus monkey that showed a very low peak-to-trough ratio. Phase III clinical trial is currently ongoing.

Peratizole is tranquillizer and antihypertensive agent.