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Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
LY-320135 is a substituted benzofuran which is structurally
distinct from the aminoalkylindole and pyrazole type
cannabinoid antagonists, AM630 and SR141716A, respectively. LY-320135 is a potent and selective canniboid CB1 receptor antagonist/inverse agonist. LY-320135 is selective (~70 fold) over canniboid CB2 receptors. LY-320135 is widely used in research, particularly for elucidating the mechanisms by which many CB1 antagonists act as inverse agonists at higher doses. LY-320135 shows weak binding to both 5-HT2 (Ki = 6.4 uM) and muscarinic receptors (Ki = 2.1 uM).
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
PBR28 or PBR-28, a chemical substance that binds to translocator protein TSPO, also known as Peripheral-type benzodiazepine receptor (PBR). TSPO located within the cells such as macrophages reaches high levels of expression in inflammatory conditions and thus can be a biomarker of neuroinflammation. When radioactivity in the form of carbon-11 is tagged to PBR 28 and is administered, its uptake in the inflammatory body regions can be measured using positron emission tomography (PET). PBR28 now is involved in a clinical trial to evaluate the specificity of its binding in the joints of patients with inflammatory joint disease, like rheumatoid and psoriatic arthritis.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Nonactin is the parent compound of macrotetrolides, a group of ionophore antibiotics produced by Streptomyces griseus. The antibacterial effects of nonactin depend upon its ability to form stable complexes with K+, Na+ or NH4 + ions and for it to support the passive diffusion of these ions across cell membranes. Nonactin has been shown to possess antitumor activity and to be an effective inhibitor of the P170-glycoprotein responsible for drug resistance in multiple drug-resistant cancer cell lines. Mitochondrial uncoupler nonactin induces apoptosis selectively in beta-catenin mutant tumor cells.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
N-Methylquipazine is a tertiary amine analog of quipazine. It binds at 5-HT3 sites with an affinity similar to that of quipazine. N-methylquipazine has a low affinity for 5-HT1A, 5-HT1B, 5-HT2, a1, a2 and muscarinic receptors. It produces a concentration-dependent increase in extracellular dopamine levels in the anterior medial prefrontal cortex. This action is dependent on the presence of Ca+2, is impulse-dependent, and depends on newly synthesized dopamine stores. The increase in the anterior medial prefrontal cortex dopamine levels by n-methylquipazine is probably, not mediated by its interaction with the 5-HT3 receptor. It might be an be an attractive candidate as a radioligand for the PET studies of 5-HT3 receptors in man.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Glyceryl 1-acetate is a glycerol ester. It potently inhibits aquaporin-mediated glycerol uptakes. Glyceryl 1-acetate was primarily used as an antidote in fluoroacetate poisoning because it was believed that acetate exerted a protective effect via competition with fluoroacetate for binding with coenzyme A. Glyceryl 1-acetate has been superseded by acetamide therapy. Glycerol 1-Acetate is a derivative of Triacetin, which is used as a food additive and flavoring.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
4-hydroxy-2-nonenal (4-HNE or HNE), a very reactive aldehyde derived from lipid peroxidation, is the product and mediator of oxidative stress. It can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. HNE is mutagenic and genotoxic because it reacts with all four DNA bases but with different efficiency: G >C > A >T. In addition, in the experiments with dogs was shown the pathophysiologic role of HNE in osteoarthritis.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Ryanodine (or ryania), a natural product found in members of the genusRyania and was previously used in insecticides. Its properties and biological actions have permitted the identification and molecular characterization of a family of intracellular Ca2+ release channels, now commonly termed the ryanodine receptors. Ryanodine binds with high affinity to the ryanodine receptors to modulate intracellular Ca2+ release, depending on the concentration used