Xylamidine is a peripherally-restricted antagonist of 5HT2A and 5HT1A receptor. It is used to study the role of the serotonin receptors in the regulation of food intake, cardiovascular function, and regulation of body temperature.

Watanidipine (AE0047) had been NDA filed for the treatment of hypertension in Japan. Watanidipine (as Calbren®) was awaiting registration with Mitsubishi Pharma Corporation in Japan. However, Mitsubishi Pharma Corporation has discontinued the development of this drug. Watanidipine had also been in phase II clinical trials for the treatment of stroke and preclinical trials for atherosclerosis. However, no recent development has been reported. Watanidipine (AE0047) has being shown to be a calcium antagonist with protective effects against cerebral ischaemia and the occurrence of stroke in several animal models.

Penfluridol is a highly potent; first generation diphenylbutylpiperidine antipsychotic was developed by Janssen Pharmaceutica in 1968 and is used to treat schizophrenial and similar psychotic disorders. It is, however, like most typical antipsychotics, being increasingly replaced by the atypical antipsychotics. This drug is long-acting dopamine receptor blocker.

Toliprolol is beta-adrenergic blocker. It was developed as antianginal and antihypertensive agent. Toliprolol is moderately lipophilic. It appears to have the appropriate characteristics for cerebral beta-adrenoreceptor imaging. However, tissue uptake of toliprolol was dominated by the nonspecific binding, both in the brain and in peripheral target organs, such as heart and lung. Toliprolol seems unsuitable for visualization of cerebral beta-adrenoceptors. After application of ethanol to mice, the content of glycogen of the liver and the brain decreased. By pretreatment with the beta-sympatholytic agent toliprolol, the ethanol-induced break-down of glycogen was partially blocked in the liver and completely abolished in the brain. In contrast, mainly synergistic effects of ethanol and toliprolol on the glycolysis of the liver and the brain were found. Toliprolol reduced the greater variance during the emotionally stressful situation in doses insufficient to diminish the mean increase in forearm blood flow.

Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Ophthalmic Bupranolol is used for the management of glaucoma and oral Bupranolol is used for the management of cardiovascular disorders. S-Bupranolol has also being shown to have superior preclinical safety profile and great antinociceptive efficacy and should be considered as a unique b-AR compound to advance future clinical pain studies.

Mefruside is a benzene disulfonamide derivative related to the benzothiadiazine or thiazide diuretics. Mefruside is adminisered orally, it is indicated for the treatment of edema and hypertension. It was developed by Bayer A.G. and is sold under the tradename Baycaron.

Dalcotidine is a histamine H2 receptor antagonist that demonstrated potent gastric mucosal protective activity on acute gastric lesions and duodenal ulcers. Dalcotidine was discontinued in phase III of clinical trials in Japan.

Efonidipine is a 1,4-dihydropyridine derivative for the treatment of hypertension and angina. Efonidipine exerts its antihypertensive and antianginal effects through blocking L- and T-type calcium channels.

Cilnidipine (FRC-8653) is a dihydropyridine (DHP) type of calcium channel antagonist. The L-type Ca2+ channel blockade by cilnidipine affects predominantly vascular smooth muscle, thereby producing vasodilation of peripheral resistance vessels and coronary arteries. The blockade of N-type Ca2+ channels affects predominantly peripheral nerve endings of sympathetic neurons, thereby dilating blood vessels by lowering plasma catecholamine levels. Furthermore, renoprotective and neuroprotective effects as well as cardioprotective action of cilnidipine have been demonstrated in clinical practice or animal examinations. Cilnidipine was originated by Fuji & Rebio Pharmaceutical Co., Ltd. and developed jointly with Ajinomoto for the treatment of hypertension. Cilnidipine has been launched in Japan.

Acetarsone is a pentavalent arsenical compound with antiprotozoal and antihelmintic properties. It was first discovered in 1921 at Pasteur Institute by Ernest Fourneau, and sold under the brand name Stovarsol (fourneau is the French word for stove). Before stovarsol was used in the treatment of congenital syphilis, it had already been used in other diseases : amoebiasis, acquired syphilis, yaws, trypanosomiasis and malaria, and a formidable list of toxic manifestations can be compiled from the literature. Bender (I927) recorded six cases of poisoning with malaise, fever, cedema, jaundice, diarrhoea, albuminuria, bronchitis, coryza and skin troubles, such as diffuse erythema, dryness and pruritus. Of 232 cases of amoebiasis treated by Brown (I935) without a death, thirteen (5.6%) had toxic erythemata, some of them so severe as to amount to exfoliative dermatitis. Although its mechanism of action is not fully known, acetarsone may bind to protein-containing sulfhydryl groups located in the parasite, thereby forming lethal As-S bonds. This may prevent their functioning and eventually kill the parasite.