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Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Acetyltryptophan, L- functions readily as a component of the food in place of the free amino acid. Acetyltryptophan, L- is a neurokinin-1 receptor antagonist. It significantly improved motor and cognitive outcomes in models of Parkinson’s diseases, as well as reduced brain edema and axonal injury in experimental traumatic brain injury and stroke. It is a potent therapeutic agent for the treatment of amyotrophic lateral sclerosis.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Imetit (S-[2-(4-(imidazolyl)ethyl]isothiourea) is a highly specific and potent histamine H3 receptor agonist. It is widely used to study H3-mediated signaling.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
β-Amyrin, a pentacyclic triterpenoid compound, that was found in many medicinal plants, including Protium heptaphyllum (Aubl.) Marchand, Catharanthus roseus (L.) G. Don, and Camellia tenuifolia (Hayata) Coh. Stuart. Several studies have reported that β-amyrin shows multiple pharmacological activities, such as the induction of angiogenesis in vascular endothelial cells and anti-inflammatory, antifibrotic, anti-apoptotic, anti-diabetic, anti-hyperlipidemic, and anti-nociceptive activities.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Himbacine is a complex piperidine alkaloid isolated from the bark of Galbulimima baccata, a species that belongs to the magnolia family. Himbacine appears to be a potent muscarinic antagonist that displays selectivity for M2 or M4 receptors, as compared to M1 or M3 receptors. Vorapaxar (SCH 530348) is a non-peptide himbacine analogue that has been developed for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction or peripheral arterial disease. Vorapaxar is a platelet inhibitor that potently and selectively inhibits thrombin-mediated platelet activation without interfering with thrombin-mediated cleavage of fibrinogen via antagonism of the platelet proteinase-activated receptor PAR1.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Panaxatriol is a triterpene sapogenin originally found in species of Panax (ginseng) that exhibits anti-inflammatory, hepatoprotective, anti-arrhythmic, and antioxidative activities. Panaxatriol increases expression of heme oxygenase 1 (HO-1) and activation of Nrf2 signaling in neurons in a PI3K/Akt-dependent manner. Panaxatriol also decreases acetaminophen-induced increases in ALT and TNF-α, preventing liver injury in vivo. Additionally, panaxatriol inhibits Ca2+ channels, decreasing channel open time and open state probability in vitro and displaying anti-arrhythmic potential. Panaxatriol is a tyrosine hydroxylase inducer. It shows neuroprotective and cardioprotective effects in vivo. Panaxatriol enhances antioxidant activity and inhibits mitochondria-mediated apoptosis. Pretreatment with ginseng total saponin, especially panaxatriol, ameliorates I/R-induced myocardial damage and this protection is caused by reducing oxidative stress. Panaxatriol can relieve myelosuppression induced by radiation injury. The abilities of regulating the expression of hemopoietic growth factor GM-CSF and promoting the maturation of bone marrow cells may be responsible for some of these beneficial effects.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
SCH-23390 is a potent and selective antagonist of the D1A and D1B dopamine receptors having Ki of 0.2 and 0.3 nM respectively. The C11 radiolabeled version has proven to be useful as a PET imaging probe in humans for the investigation of a number of neurological conditions including Schizophrenia, Parkinson's Disease, and Huntington's Disease. It should be noted that the non-radiolabeled compound did receive preclinical interest as a potential therapeutic (annotated separately), although such efforts have been discontinued due to side-effects and a lack of therapeutic efficacy.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Theaflavin is a black tea polyphenol, which possesses a wide variety of pharmacological properties including potent antioxidative, anti-apoptotic, anti-cancer and anti-inflammatory effects. Theaflavin (TF-1) can bind to, and inhibit the purified 20S proteasome, accompanied by suppression of tumour cell proliferation, suggesting that the tumour proteasome is an important target whose inhibition is at least partially responsible for the anticancer effects of black tea. Theaflavin is a potent inhibitor of interleukin-8 gene expression in vitro. The proximal mechanism of this effect involves, in part, inhibition of IkappaB kinase activation and activator protein-1 pathway. Theaflavin has been known to possess neuroprotective effects against ischemia, Alzheimer's disease and other neurodegenerative disorders.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Salsolinol (1-methyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline, SAL) is a tetrahydroisoquinoline derivative, detected in humans. Salsolinol can be formed in the mammalian brain by three different mechanisms: (1) via the nonenzymatic Pictet–Spengler condensation of dopamine and aldehydes producing salsolinol as two racemic isomers (R or S). (2) By the nonenzymatic condensation of dopamine and pyruvate yielding 1-carboxyl-tetrahydroisoquinoline, followed by decarboxylation and reduction, which produces (R)-salsolinol. (3) By selective synthesis of (R)-salsolinol from dopamine and acetaldehyde, the level of which is increased after ethanol intake. Apart from that salsolinol has also been detected in certain beverages and foodstuff, including soy sauce, cheese. Only the (R) enantiomer of Salsolinol and occur in the human brain, cerebrospinal fluid (CSF) and intraventricular fluid (IVF), and the (S) enantiomer was not detected. Salsolinol was also found to be involved in neurotoxicity processes altering the normal function and survival of dopamine neurons. It has been proposed, that salsolinol participated in the etiopathogenesis of Parkinson’s disease. Salsolinol could inhibit various enzymes, for example, monoamine oxidase and tyrosine hydroxylase and recently was revealed, that (R)-SAL and (S)-SAL were agonists of the μ-opioid receptor. (S)-SAL is a more potent agonist than the (R)-SAL stereoisomer, it was suggested that an opioid action of SAL or its enantiomers is involved in the rewarding effects of ethanol.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
LY-450108 had been in phase I clinical trial by Lilly, where was shown, that this drug safe and well tolerated in healthy subjects. This drug in the preclinical studies on animal models for the treatment of depression and Parkinson's disease.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
CALCIUM PHYTATE is a calcium salt of phytic acid (also known as myo-inositol hexakisphosphate (IP6), inositol polyphosphate), which is a strong chelator (complexing agent) of important minerals such as calcium, iron. In nature, it functions as storage for phosphorus in plants, especially in the hulls of nuts and seeds. Phytic acid (IP6) for a long period was considered an antinutritional factor. However, in vitro and in vivo studies have demonstrated its beneficial effects in the prevention and treatment of several pathological conditions and cancer. It also exhibits protective action in Parkinson's disease and this is correlated with its anti-inflammatory effect, which may be associated with suppression of pathways that involved in NF-κB and p-ERK. In addition was discovered, that phytic acid might provide a viable treatment option for Alzheimer's disease.