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Status:
Possibly Marketed Outside US
Source:
Unknown
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Potassium Glycerophosphate is a source of potassium. It is used in the treatment of nutritional deficiencies. Potassium supplements can be an important part of the recovery from or prevention of many different ailments and diseases. The most common of these include helping lower blood pressure and serving as a stroke preventative. Potassium can also be used to lower levels of calcium, to help with certain diseases including Alzheimer’s and Meniere’s. It may also help with some more common issues such as a common allergy, migraines, heavy acne, alcohol abuse, dizziness and confusion, extreme fatigue, recurring constipation, insomnia, anger and aggression, irregular heartbeat and stress. Potassium can either be taken as a supplement by mouth or it can be given intravenously to certain patients who require a faster dosing of the mineral or cannot take it orally.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Propentofylline is a selective inhibitor of adenosine transport and phosphodiesterase. For several years it has been well established in the geriatric therapy of the dog improving hemodynamics in cerebral and peripheral compartments. In human medicine clinical development of this pharmaceutical has already entered an advanced stage for the long-term therapy of patients with Alzheimer's disease and vascular dementia. In the brains of senile dogs and in human patients suffering from Alzheimer's disease comparable neuropathological findings can be made. In experimental models of vascular dementia and/or Alzheimer's disease it improves cognitive functions, inhibits inflammatory processes as well as excessive activation of microglia, formation of free radicals, cytocines and abnormal amyloid precursor proteins (APP). It stimulates synthesis and liberation of nerve growth factor (NGF) and reduces ischemic damage to the brain. In clinical studies in humans it improved cognitive functions as well as global functions and the ability to cope with tasks of routine daily life in patients suffering from Alzheimer's disease and vascular dementia. Possible mechanisms of action include a direct glial modulation to decrease a reactive phenotype, decrease glial production and release of damaging proinflammatory factors, and enhancement of astrocyte-mediated glutamate clearance. Net effects of propentofylline in vivo will be dependent on the concentrations of propentofylline and adenosine available and on the subtypes of adenosine receptors, phosphodiesterases, and nucleoside transporters present. In March, 2000 Aventis Pharma, announced that was discontinuing development of propentofylline as a possible treatment for Alzheimer's disease. The decision was a result of the company's portfolio review process which is intended to ensure that resources are devoted only to projects with a high potential for success.
Status:
Possibly Marketed Outside US
Source:
NCT02020408: Phase 4 Interventional Completed Eating Disorder
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Raclopride is a salicylamide neuroleptic, that acts as a selective antagonist of D2 dopamine receptors both in vitro and in vivo. Tritium-labelled raclopride has properties that demonstrate its usefulness as a radioligand for the labelling of dopamine-D2 receptors : 3H-Raclopride has a high affinity for the rat and human dopamine-D2 receptors, the non-specific binding of 3H-raclopride is very low, not exceeding 5% of the total binding and the distribution of the 3H-raclopride binding sites in the brain closely correlates with the dopaminergic innervation. The binding of 3H-raclopride is blocked by dopamine-D2 agonists and antagonists, while the D1 agonist SKF 38393 and the Dl antagonist SCH 23390 have much less potency. The interaction of dopamine with 3H-raclopride binding results in a shallow competition curve, which suggests that 3H-raclopride, similar to other dopamine-D2 radioligands, labels both high and low agonist affinity states of the dopamine-D2 receptor. The in vivo receptor binding studies performed with 3H-raclopride also demonstrate its favorable properties as a dopamine-D2 receptor marker in vivo In contrast to some other compounds used as radioligands, raclopride enters the brain readily and binds with a low component of non-specific binding in all dopamine-rich brain areas. A saturation curve may be achieved in vivo binding studies since injections of increasing concentrations of 3H-raclopride appears to be saturated at concentrations above 25 mkCi (corresponding to approximately 5 nmol/kg). Raclopride antagonizes apomorphine-induced hyperactivity in the rat at low doses (ED50 = 130 nM/kg i.p.) but induces catalepsy only at much higher doses (ED50 = 27 mkM/kg i.p.). Radiolabelled raclopride has been used as a ligand for in vitro and in vivo autoradiography in rat and primate brains. Raclopride C 11 is used with positron emission tomography (PET) as a clinical research tool to determine dopamine type 2 (D 2) receptor density in the human brain under normal and pathological conditions. For example, raclopride C 11 used in PET studies has served to confirm the age-related decrease in striatal dopamine D2 receptor density, which may be associated with a decline in the motor as well as cognitive functions. In patients with Alzheimer's disease, raclopride C 11 may be used to examine neuroreceptor distribution and quantities, which may help in the analysis of degenerative alterations of neuron populations and neuroreceptor systems in patients with this disease. In Huntington's disease, in which degeneration of neostriatal interneurons occurs (postsynaptic to the dopaminergic input), specific binding of raclopride C 11 to D 2 receptors may serve as one of the parameters in predicting performance in cognitive tasks.
Status:
Possibly Marketed Outside US
Source:
Largon by Klinge
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Kavain is the main kavalactone found mostly in the roots of the kava plant. Kavain interacts with voltage-dependent Na+ and Ca2+ channels, GABAA ion channels. Kavain is found to be involved in TNF-alpha expression in human and mouse cells via regulation transcriptional factors. Kavain exhibits neuroprotective effects in models of Alzheimer's and Parkinson's diseases, and produces anxyolitic effect.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Loganin was found in parts of some trees and shrubs including bark of Mastixia arborea (Cornaceae family), Corni fructus and A. boonei (Apocynaceae), a West African herbal medicinal plant traditionally used for its antimalarial, aphrodisiac, antidiabetic, antimicrobial properties. A key intermediate in the biosynthesis of indole alkaloids loganin was synthesized in 1971 by carboxyl group methylation of loganic acid. It has been shown, that loganin possesses anti-shock effects, anti-oxidant, glucose-lowering and neuroprotective properties. Loganin exhibits an anti-inflammatory effect in cases of acute pancreatitis and its pulmonary complications through inhibition of NF-κB activation. It is an active ingredient of a new herbal formula KBMSI-2 which has been through Phase 4 clinical trial for the efficacy and safety in the treatment of Erectile Dysfunction. Loganin inhibits β-secretase in vitro and increases performance in Morris water maze and Y-maze tests in vivo, suggesting potential benefit in memory impairment and Alzheimer’s disease. In addition, it also modulates ERK signaling to decrease connective tissue growth factor (CTGF) and downregulates expression of MCP-1, NF-κB, and iNOS in animal models. Inhibition of CTGF may be a potential target in diabetic nephropathy (DN) therapy, which highlights the possibility of using loganin to treat DN.
Status:
Possibly Marketed Outside US
Source:
Besipirdine hydrochloride
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Besipirdine is a potential novel first-in-class oral treatment for over active bladder currently in Phase II development, with a mechanism of action clearly different from that of antimuscarinics. It was under evaluation by Aventis up to phase III for Alzheimer’s disease, involving the administration of the compound to over 1500 patients. However, this research has been discontinued. Besipirdine antagonizes alpha-2 and alpha-1 adrenoceptors and inhibits both norepinephrine and serotonin uptake. The most common adverse events were asymptomatic postural hypotension and asymptomatic bradycardia.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Trichlorfon (Metrifonate), the organophosphorous cholinesterase inhibitor, O,O-dimethylhydroxy-2,2,2-trichlorethyl-phosphonate, has been used sporadically in the treatment of human schistosomiasis for a decade. It has selective and variable schistosomicidal activity against S. haematobium that results from its partial metabolism to a highly active anti-cholinesterase, dichlorvos. Schistosomal cholinesterase is more susceptible to this metabolite than that of the human host, but transient reductions in both plasma and erythrocyte cholinesterase activity are demonstrable at therapeutic dosage. However, despite early concerns about its potential toxicity, metrifonate is well tolerated and has been used effectively and extensively in large-scale control programmes. Its potential to enhance central nervous system cholinergic neurotransmission led to clinical trials for the treatment of people with Alzheimer's disease (AD).
Status:
Possibly Marketed Outside US
Source:
SM 10.888 by Sumitimo JPN
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Velnacrine (9-amino-1,2,3,4-tetrahydroacridin-1-ol) is an inhibitor of acetylcholinesterase. It was studied for the treatment of Alzheimer's disease however development was discontinued. There has been no research into the use of velnacrine as a cognitive enhancer in the treatment of Alzheimer's disease since 1994. The FDA peripheral and CNS drug advisory board voted unanimously against recommending approval. This review shows the toxic nature of velnacrine, and provides no evidence of efficacy.
Status:
Possibly Marketed Outside US
Source:
NCT02027337: Phase 4 Interventional Unknown status Polycystic Ovarian Syndrome
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Cyproterone belongs to a group of medications known as steroidal antiandrogens. It suppresses testosterone and its metabolites. It has approximately three-fold lower potency as an antagonist of the androgen receptor relative to cyproterone acetate. Cyproterone acetate is used to treat advanced prostate cancer and acne.
Status:
Possibly Marketed Outside US
Source:
NCT02931136: Phase 4 Interventional Not yet recruiting Mild Cognitive Impairment
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Huperzine A is a plant alkaloid derived from Club moss plant, Huperzine serrata, which is a member or the Lycopodium species. Huperzine-A is in phase III clinical trial in the USA (Alzheimer disease) and is available as a dietary supplement. It selectively and reversibly inhibits acetylcholinesterase. Huperzine A is also a NMDA receptor antagonist, which protects the brain against glutamate induced damage, and it increases nerve growth factor levels. Huperzine A is used for Alzheimer's disease, memory and learning enhancement, and age-related memory impairment. It is also used for treating a muscle disease called myasthenia gravis, for increasing alertness and energy, and for protecting against agents that damage the nerves such as nerve gases. It can cause some side effects including nausea, diarrhea, vomiting, sweating, blurred vision, slurred speech, restlessness, loss of appetite, contraction and twitching of muscle fibers, cramping, increased saliva and urine, inability to control urination, high blood pressure, and slowed heart rate. Various medications used for glaucoma, Alzheimer's disease, and other conditions (Cholinergic drugs) interacts with Huperzine A.