Tiamenidine (also known as HOE 440) is a diazacycloalkene derivative patented by Farbwerke Hoechst A.-G. as 2 alpha-sympathomimetic antihypertensive agents. In preclinical models, tiamenidine induces hypotension and bradycardia in renal hypertensive cats and rats and in normal rats and dogs. Furthermore, Tiamenidine inhibits the liberation of norepinephrine from nerves leading to the heart and suppress sympathetic circulatory reflexes in dogs. In clinical trials, Tiamenidine exerts favor influences on systolic and diastolic blood pressure, and reduces plasma noradrenaline and adrenaline levels and suppresses plasma renin activity. Unfortunately, during the withdrawal of Tiamenidine, there is a rebound of blood pressure and plasma noradrenaline and adrenaline, overshooting baseline levels.

Tiapamil (also known as Ro 11-1781) is a dithiane derivative patented by Hoffmann-La Roche, F., und Co., A.-G. as calcium-channel antagonist useful for myocardial infarction treatment. Tiapamil, like verapamil, inhibited in a concentration-dependent manner Ca2+-induced contractions in isolated, K+-depolarized preparations of rat renal artery, dog coronary artery and rabbit main pulmonary artery. The inhibitory effects of Tiapamil can be overcome by raising the Ca2+ concentration of the bath fluid. In the rabbit main pulmonary artery, Tiapamil reduces 45Ca influx into the K+-depolarized vascular smooth muscle cells. Tiapamil inhibits the slow potentials in partially depolarized guinea-pig papillary muscles. Tiapamil decreases contractile force in isolated guinea-pig atria and papillary muscles, as well as in isolated cat hearts. Tiapamil also reduces heart rate and increases coronary flow in these preparations. Tiapamil doubled coronary artery blood flow in the coronary sinus blood without producing major changes in blood pressure and heart rate in anesthetized dogs. Tiapamil did not affect contractions of isolated guinea-pig ileum, rat stomach strips or rat vas deferens in response to various stimulants. Tiapamil have no major effects on renal water and electrolyte excretion, on autonomic nerves and receptors, on pain perception and on the central nervous system. Acute, subacute, and chronic toxicity studies demonstrate low toxicity for Tiapamil with no tendency for accumulation. In clinical trials, Tiapamil effectively lowers systolic and diastolic blood pressure, but have no effects on heart rate

Sergolexole [LY 281067] is an ergoline ester similar in structure to amesergide [LY 237733], with potent and highly selective antagonist activity at serotonin 2. The preclinical pharmacologic activity of LY 281067 shows it to be a potent and highly selective serotonergic (5-HT2) receptor antagonist. Based upon binding studies with 5-HT2 receptors in brain cortical membranes and block of 5-HT-induced contractions in the rat jugular vein, LY 281067 showed high affinity at 5-HT2 receptors with a dissociation constant of approximately 1 nM. LY 281067 was a highly selective 5-HT2 receptor antagonist without appreciably binding to 5-HT1, D1 or D2 receptors or interacting with histamine (H1), cholinergic, beta adrenergic or alpha-1 adrenergic receptors in smooth muscle. LY 281067 had modest affinity at alpha-2 receptors with a dissociation constant of approximately 100 nM. Oral bioavailability of LY 281067 in spontaneously hypertensive rats was excellent with an oral to i.v. dose ratio approximating 4. Sergolexole was undergoing phase II clinical trials with Eli Lilly in the USA as a potential treatment for migraine and anxiety, but development of this compound, but development of this compound has been discontinued.

Quindecamine (also known as UCL-1407) is quinaldine derivative with antibiotic and fungicidal activity. Treatment of rats and mice with Quindecamine (250 mg/kg/ day) each day for 4 weeks followed by 500 mg/kg/day for 2 more weeks reduced spontaneous motility and body weight but produced no pathological abnormalities of the various organs studied. In vitro, the drug showed very good activity against Staphylococcus aureus, Streptococcus hemolyticus, Candida albicans, Trichophyton mentagrophytes, and T. vaginalis. The drug had very good activity in 180 human subjects with various bacterial and mycotic diseases of the skin and mucosa when applied as a 1% salve.

Deterenol is a beta-adrenoceptor agonist. It is an effective nonmydriatic and nonmiotic hypotensive agent, which can be used in antiglaucoma treatment.

Lysergide (LSD) is a semi-synthetic hallucinogen and is one of the most potent drugs known. Recreational use became popular between the 1960s to 1980s, but is now less common. LSD was first synthesized by Albert Hoffman while working for Sandoz Laboratories in Basel in 1938. Some years later, during a re-evaluation of the compound, he accidentally ingested a small amount and described the first ‘trip’. During the 1950s and 1960s, Sandoz evaluated the drug for therapeutic purposes and marketed it under the name Delysid®. It was used for research into the chemical origins of mental illness. Recreational use started in the 1960s and is associated with the ‘psychedelic period’. LSD possesses a complex pharmacological profile that includes direct activation of serotonin, dopamine and norepinephrine receptors. In addition, one of its chief sites of action is that of compound-specific (“allosteric”) alterations in secondary messengers associated with 5HT2A and 5HT2C receptor activation and changes in gene expression. The hallucinogenic effects of LSD are likely due to agonism at 5HT2A and 5HT2C receptors. LSD is also an agonist at the majority of known serotonin receptors, including 5HT1A, 5HT1B, 5HT1D, 5HT5A, 5HT6 and 5HT7 receptors. During the 1960s, LSD was investigated for a variety of psychiatric indications, including the following: as an aid in treatment of schizophrenia; as a means of creating a "model psychosis"; as a direct antidepressant; and as an adjunct to psychotherapy. LSD is listed in Schedule I of the United Nations 1971 Convention on Psychotropic Substances.

Becanthone is an antischistosomal agent possesses the ability to inhibit tumors.

Harmine (aka telepathine) is a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds. It is a naturally occurring metabolite in a number of plants, notably the Middle Eastern plant harmal or Syrian rue (Peganum harmala) and the South American vine Banisteriopsis caapi. Harmine is a reversible inhibitor of monoamine oxidase A (MAO-A), but not MAO-B. Harmine has been found to have potential anti-cancer and neuroprotective properties, and also promotes differentiation of osteoblasts and chondrocytes while inhibiting osteoclastogenesis. Harmine has also been used as a C-11 labeled probe in positron emission tomography.

Lysergide (LSD) is a semi-synthetic hallucinogen and is one of the most potent drugs known. Recreational use became popular between the 1960s to 1980s, but is now less common. LSD was first synthesized by Albert Hoffman while working for Sandoz Laboratories in Basel in 1938. Some years later, during a re-evaluation of the compound, he accidentally ingested a small amount and described the first ‘trip’. During the 1950s and 1960s, Sandoz evaluated the drug for therapeutic purposes and marketed it under the name Delysid®. It was used for research into the chemical origins of mental illness. Recreational use started in the 1960s and is associated with the ‘psychedelic period’. LSD possesses a complex pharmacological profile that includes direct activation of serotonin, dopamine and norepinephrine receptors. In addition, one of its chief sites of action is that of compound-specific (“allosteric”) alterations in secondary messengers associated with 5HT2A and 5HT2C receptor activation and changes in gene expression. The hallucinogenic effects of LSD are likely due to agonism at 5HT2A and 5HT2C receptors. LSD is also an agonist at the majority of known serotonin receptors, including 5HT1A, 5HT1B, 5HT1D, 5HT5A, 5HT6 and 5HT7 receptors. During the 1960s, LSD was investigated for a variety of psychiatric indications, including the following: as an aid in treatment of schizophrenia; as a means of creating a "model psychosis"; as a direct antidepressant; and as an adjunct to psychotherapy. LSD is listed in Schedule I of the United Nations 1971 Convention on Psychotropic Substances.

Mixidine is negative chronotropic agent patented by McNeil Laboratories. Mixidine produced a dose-related decrease in heart rate elevated reflexly by aminophylline, by beta-adrenergic stimulation induced by isoproterenol, by sympathetic nerve stimulation and by intravenous infusion of glucagon. Mixidineattenuated the increase in contractile force produced by sympathetic nerve stimulation but not that induced by isoproterenol. The compound antagonized the increase in the rate of isolated guinea-pig atria induced by both isoproterenol and histamine. In the conscious dog, Mixidine caused no decrease in resting heart rate, mean arterial pressure and cardiac output. It reduced atropine-induced sinus tachycardia as well as that induced by treadmill exercise.