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Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
5-carboxamidotryptamine (5-CT) is a 5-HT1 agonist with high affinity at 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5 and 5-HT7 receptors. As one of the first compounds reported active at 5-HT1B, 5-carboxamidotryptamine was originally investigated as a potential treatment for migraine. During preclinical studies, 5-CT was found to cause vasodilatation of carotid circulation and hypotension in animals, effects that were later attributed to potent agonist activity at 5-HT7. Subsequent structural modifications of 5-CT led to the discovery of the anti-migraine drug sumatriptan. 5-CT is primarily used as a pharmacological tool for study of 5-HT1 and 5-HT7 mediated functional responses.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Phenyl biguanide (phenylbuguanide, PBG) is a 5-hydroxytryptamine receptor 3 agonist used to study the role of serotonin receptors in the central nervous system. It has been found to trigger dopamine release in the nucleus accumbens of rats. Phenylbiguanide is used to make amanozine.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Cyclopiazonic acid (CPA) is an indole tetramic acid mycotoxin produced by Aspergillus and Penicillium species.
The toxicity of CPA is attributed to its ability to alter normal intracellular calcium flux through the specific inhibition of sarcoplasmic or endoplasmic reticulum calcium-dependent ATPase (SERCA) essential for calcium uptake as in the muscle contraction-relaxation cycle, which results in increased muscle contraction. Beside colonizing various grains and seeds, these molds can grow on many food substrates, such as cheese and meat products. Therefore, CPA can contaminate a number of agricultural commodities, animal feeds, and food sources. This toxin has been found in edible tissue in poultry, milk, and eggs presumptively due to animals’ consumption of contaminated feeds. Despite the wide presence of CPA, few incidents of animal mycotoxicosis and no confirmed incident of human poisoning have been attributed to CPA. In preclinical models CPA demonstrated anti-arrhythmic effects.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
The pyrrolizidine alkaloid senecionine has been shown to produce an increase in cytosolic free Ca2+ concentration in isolated hepatocytes that correlated with an increase in cellular toxicity. Senecionine inhibits the sequestration of Ca2+ in extramitochondrial and mitochondrial compartments possibly by inactivating free sulfhydryl groups and oxidizing pyridine nucleotides respectively. Senecionine showed moderate antitrypanosomal activity with an IC50 value of 41.78 ug/ml.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
2'-CH3-MPTP is an extremely potent dopaminergic neurotoxin, which lead to large decrements in the neostriatal concent of DA and a large loss in the capacity of a neostriatal synaptosomal preparations to take up [3H]DA. 2'CH3-MPTP-induced neurotoxicity, was attenuated by pretreatment of mice with dopamine uptake inhibitor, and non-specific MAO-A and MAO-B inhibitor, but not by a specific MAO-B inhibitor. The mechanism of toxicity is formation of a metabolite 2'CH3-MPP+, which is a potent inhibitor of mitochondrial respiration.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Citreoviridin (CIT) is a mycotoxin produced by Penicillum citreonigrum, Aspergillus terreus and Eupenicillium ochrosalmoneum. CIT occurs naturally in moldy rice and corn. CIT is associated with the development of atherosclerosis in the general population. Citreoviridin displays the ability to potently inhibit mitochondrial ATPases via uncompetitive inhibition of ATP hydrolysis. Additional research shows that Citreoviridin can inhibit ATP-driven reduction of NAD+ by succinate and ATP driven NAD transhydrogenase in ox hearts. Citreoviridin inhibits both membrane-bound and soluble mitochondrial ATPases. In particular, it inhibits synaptosomal Na+/K+-ATPase, altering synaptic transmission, and binds to the beta subunit of F1-ATPAse. As a result it has been shown to inhibit mitochondrial energy-linked reactions such as ADP-stimulated respiration, ATP-driven reduction of NAD + by succinate, and ATP-driven NAD transhydrogenase. Mycotoxins are often able to enter the liver and kidney by human organic anion transporters (hOATs) and human organic cation transporters (hOCTs). They can also inhibit uptake of anions and cations by these transporters, interfering with the secretion of endogenous metabolites, drugs, and xenobiotics including themselves. This results in increased cellular accumulation of toxic compounds causing nephro- and hepatotoxicity. citreoviridin could
specifically kill cancer cells but not normal cells because of
ectopically expressed ATP synthase (ecto-ATP synthase) on
plasma membrane of cancer cells.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Imidazenil is an imidazo-benzodiazepine derivative with high intrinsic efficacy and selectivity for α2-, α3-, and α5- but low intrinsic efficacy for α1-containing GABA(A) receptors. It has an unusual profile of effects, producing some of the effects associated with normal benzodiazepines such as anticonvulsant and anxiolytic effects, yet without any notable sedative or amnestic effects. It has been suggested as a safe and effective treatment for anxiety, a potent yet non-sedating anticonvulsant and as a novel treatment for schizophrenia.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Anabasine, a tobacco alkaloid, was used as a biomarker of active tobacco use. Anabasine is a selective alpha7-nicotinic acetylcholine receptor agonist. Anabasine antagonized MK-801-elicited mouse popping behavior, an animal model of schizophrenia.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
2-methyl-4,6-dinitrophenol (4,6-Dinitro-ortho-cresol, DNOC) is a yellow crystalline solid. DNOC is used agriculturally as a larvicide, ovicide and insecticide (against locusts and other insects) as well as a potato haulm desiccant. It
is also used as a polymerization inhibitor and as an intermediate in the chemical industry. For agricultural uses, DNOC is mainly formulated as emulsifiable concentrate, either aqueous or oily. 4,6-Dinitro-o-cresol is an uncoupler of the mitochondrial respiratory system. It causes an increase in basal metabolic rate with raised temperature and weight loss in man and animals. After metabolic activation, 4,6-dinitro-o-cresol has mutagenic potential in vitro. In vivo, evidence of clastogenic effects was obtained with a herbicide containing 4,6-dinitro-o-cresol but not with the pure substance. A long-term study with rats yielded no evidence of carcinogenic effects. During the 1930s, DNOC, along with dinitrophenol, was used therapeutically as a
weight-loss agent after animal experiments had demonstrated that dinitrophenols increased the
basal metabolic rate (BMR). The earliest mention of the use of these compounds for weight loss
is a publication by Cutting and Tainter (1933) in which the authors reported clinical studies of
dinitrophenol for this purpose. Dodds and Robertson (1933) reported that the related compound,
DNOC, exhibited a greater effect on metabolism than dinitrophenol, leading to the marketing of
DNOC for weight loss. Following the publication of these reports, dinitrophenol, and to a lesser
extent, DNOC, began selling in drug stores and was prescribed by physicians for weight loss. DNOC acts mainly as an
inhibitor of oxidative phosphorylation at the mitochondrial level, inducing
a significant increase in basal metabolism and hyperthermy. The oxidation
of carbohydrate forms the main source of energy of the body and the
energy is “stored” in the form of compounds containing phosphate (high
energy phosphate bonds of adenosine triphosphate or ATP). This
compound is then a source of energy to the body. DNOC inhibits the
formation of ATP. In the presence of DNOC the oxidative process
continues and is even increased, but the energy cannot be converted to a
useable form and it is therefore dissipated as heat. In muscle ATP cannot
be re-synthesized and is progressively broken down to adenylic acid. The
shortage of ATP may lead to muscular paralysis which for critical organs,
such as heart and respiratory muscles, includes a blocking of their vital
functions and in the case of death by DNOC poisoning, to early rigor mortis.
2-Ethoxyethyl acetate (2-EEA) is a colourless liquid with a fruity smell at room temperature and normal pressure. 2-Ethoxyethyl acetate belongs to the group of glycol ethers
which are mainly used as solvents. 2-EEA was mainly used as a solvent in the chemical industry and for the formulation of paints, lacquers and varnishes for industrial use.
2-EEA was also used as an intermediate in the chemical industry.