Firategrast (SB683699) is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS), that had been studied in phase II trials at GlaxoSmithKline under a license from Mitsubishi Tanabe Pharma for the oral treatment of multiple sclerosis (MS) in Europe. GlaxoSmithKline and Tanabe Seiyaku (now Mitsubishi Tanabe Pharma) had been studying the drug candidate for the treatment of asthma, rheumatoid arthritis (RA) and Crohn’s disease, but these studies had being discontinued. Firategrast is a drug for the treatment of multiple sclerosis (MS) which is found to be caused by the migration of leucocytes (such as monocytes, T cells, B cells and dendritic cells) into CNS. And the integrin α4β1 is found to take participate in the migration through activating the leucocytes. Firategrast has a much shorter half-life than natalizumab with about 2.5 hours to 4.5 hours. It is found to inhibit the binding of the integrins to the associated ligands, including vascular cell adhesion protein 1 and mucosal addressin cell adhesion molecule 1. In CNS, firategrast treatment caused moderate decreases of total lymphocyte count, lymphocyte subset count and the ratio of CD4 to CD8. In peripheral blood, firategrast treatment resulted in the increases of total lymphocyte count, all lymphocyte subset count as well as the peripheral CD34+ early haematopoietic progenitor cell count. Firategrast was well tolerated at the maximum doses of 1200 mg for men and 900 mg for women. Firategrast showed no side effects, such as PML or JC-virus reactivation, at these doses. In Phase I clinical trials, the administration of firategrast significantly reduced the cumulative number of new gadolinium-enhancing lesions in patients with relapsing remitting MS.

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.

Prorenoate Potassium is a water-soluble synthetic aldosterone antagonist patented by Merck and Co., Inc. as an antihypertensive agent. In preclinical studies a significant natriuretic response was obtained at dosages of 1 mg/kg and approximately 1.8 mg/kg in the dog and rat, respectively. Prorenoate is relatively inactive at the renal level in adrenalectomized rats without mineralocorticoid replacement. Prorenoate possesses no more than 2% of the natriuretic activity of hydrochlorothiazide in the intact animal. Clearance studies in dogs indicate a direct renal tubular site of interaction between prorenoate and aldosterone independent of changes in renal hemodynamics. The natriuretic response occurred within 100 minutes after a single oral dose and was sustained for at least 7 hours. In clinical trials Prorenoate reversing the renal effects of the synthetic mineralocorticoid fludrocortisone in healthy individuals. Prorenoate was significantly more potent in retaining K+ than in increasing Na+ excretion.

Dioxifedrine is the putative metabolite of 3,4-methylenedioxymethamphetamine. It is the sympathomimetic agent and beta-2 -adrenergic agonist with bronchodilator activity. Dioxifedrine selectively binds to and activates beta-2 adrenergic receptors in bronchiolar smooth muscle, thereby causing stimulation of adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased intracellular cAMP levels cause relaxation of bronchial smooth muscle. In stimulatory studies dioxifedrine increased locomotor activity from 15 to 30 min following the drug administration. Following intracerebroventricular injection dioxifedrine rapidly reduced blood pressure and heart rate.

Ortetamine, also known as 2-methylamphetamine, is a monoamine releaser that was studied as a stimulant drug. Information about the current use of this drug is not available.

Nafcaproic acid (DA-808) is a synthetic choleretic agent.

Nylestriol is a synthetic estrogen which is marketed in China under the brand name Wei Ni An. Nylestriol can be used as an effective and acceptable estrogen replacement therapy for postmenopausal women. It was found to be effective, safe and convenient in treating postmenopausal osteoporosis.

Bipenamol is a benzenemethanol derivative used to prepare novel semicarbazide-derived inhibitors of human dipeptidyl peptidase I.