Lurosetron (GR 87442) is a serotonin 5HT3 receptor antagonist. It was undergoing clinical evaluation with Glaxo Wellcome in the UK as a potential drug for the treatment of emesis.

Tolafentrine is phosphodiesterase 3/4 (PDE3/4) inhibitor. Treatment of endothelial cells with tolafentrine significantly decreased asymmetrical dimethylarginine-induced apoptosis via a cAMP/PKA-dependent pathway by induction of dimethylarginine dimethylaminohydrolase 2 (DDAH2). Chronic nebulization of PDE3/4 inhibitor significantly attenuated monocrotaline-induced hemodynamic, gas exchange abnormalities, vascular remodeling, and right heart hypertrophy. When chronically nebulized from day 28 to 42 (12 daily aerosol maneuvers), after full establishment of severe pulmonary hypertension, tolafentrine reversed about 60% of all hemodynamic abnormalities in rats, right heart hypertrophy and monocrotaline-induced structural lung vascular changes, including the proportion of pulmonary artery muscularization. Tolafentrine was developed as therapeutic agent for the treatment of asthma. However, this development was discontinued.

Valtrate is a principle compound isolated from Valeriana jatamansi Jones, which is a Traditional Chinese Medicine used to treat various mood disorders. Valtrate at a high dose has been found to have sedative properties by inhibiting spontaneous motion and increasing the sleeping number induced by pentobarbital sodium in mice. In rats valtrate exhibits anxiolytic-like profiles in the elevated plus maze test and the open field test. Valtrate attenuated HPA axis activity by reducing the corticosterone level. Valtrate also possesses anti-breast cancer activities via cell cycle arrest, apoptosis, and inhibition of cell migration, thus supporting valtrate as a potential antitumor agent.

Tolmesoxide is a member of a series of aryl sulphoxides, which were synthesized as potential anti-hypertensive agents. Studies in rats indicate that tolmesoxide lowers blood pressure by a direct relaxant effect on vascular smooth muscle. Tolmesoxide is approximately equipotent in dilating arterioles and noradrenaline constricted veins. Thus, tolmesoxide should be classified as a non-selective vasodilator. Tolmesoxide, in common with other vasodilators, has a short half-life, probably due to rapid metabolism as indicated by the early appearance of the major metabolite in the plasma. However, the relatively long duration of action (up to 12 h) contrasts with the short half-life and suggests that tolmesoxide has a specific mechanism of action of relatively long duration in the vascular walls in a manner suggested for hydralazine and minoxidil. The bioavailability of oral tolmesoxide from capsules averaged 84.5% and was independent of dose. Described side effects are: facial flushing, severe nausea, headaches and palpitations.

Volazocine was studied as an analgesic. Information about the current use of this agent is not available.

Tolquinzole is an antidepressant agent.

Tiprostanide is a 13-thia-PGE1 analog which also contains a p-benzamidophenyl ester, presumably to enhance crystallinity and stability. Although originally targeted and evaluated as an antihypertensive agent, emphasis was switched to an antiulcer indication because of disappointing clinical results. Tiprostanide has two distinct properties in the human stomach, viz. antisecretory and protective, which are independent of each other. Antisecretory prostaglandins protect the human stomach against aspirin and bile salts in doses which are much smaller than the threshold antisecretory ones.

Truxipicurium, a derivative of alpha-truxillic acid, a curare-like drug, is a neuromuscular blocking agent with rigid structure.

Vinepidine, a derivative of vincristine participated in clinical trials as an antineoplastic agent. As a result, the extreme neuromuscular toxicity was observed, that is why this study was discontinued.

Indoxole is methoxyphenyl-indole derivative and cyclooxygenase inhibitor with potent anti-inflammatory activity. Indoxole is effective against carrageenin-induced edema in intact and adrenalectomized rats and in mice and gerbils. Oral potency varies from 0.9 to 5.0 times that of phenylbutazone and 3 to 15 times that of acetylsalicylic acid, depending upon the vehicle employed. In prevention and therapy of rat adjuvant arthritis, Indoxole is equipotent to phenylbutazone and more potent than acetylsalicylic acid. It does not produce water and electrolyte retention, thymolysis, adrenal hypertrophy, gastric ulcers, and slow reacting substance-anaphylaxis and bradykinin inhibition characteristic of phenylbutazone. Its spectrum of antiinflammatory and pharmacologic activity is narrower than that of hydrocortisone. Pharmacologically, it is similar to acetylsalicylic acid. Indoxole lowers yeast-induced fever in rats, prevents Proteus mirabilis-induced fever in dogs, inhibits phenylquinone-induced writhing in mice and increases the pain threshold in rats.