GW311616 hydrochloride is a chemical compound that has gained significant attention in the scientific community due to its potential therapeutic and environmental applications. It is a selective antagonist of the CB1 receptor, which is involved in the regulation of appetite, pain, and mood. This paper aims to provide a comprehensive review of GW311616 hydrochloride, including its method of synthesis or extraction, chemical structure and biological activity, biological effects, applications, and future perspectives and challenges.
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GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM; free base form of GW311616A.IC50 value: 22 nM [1]Target: neutrophil elastaseThe HNE inhibitor GW311616A is selective over other human serine proteases (IC50 values >100 uM for trypsin, cathepsin G, and plasmin, >3 mM for chymotrypsin and tissue plasminogen activator). Acetylcholinesterase is not inhibited by GW311616A at 100 uM.GW311616A is more potent than thetrifluoromethylketone inhibitor ZD8321 (Ki=13 nM). GW311616A is orallybioavailable in rat, dog (Table 4) and hamster despite moderate to high plasma clearance, which indicates that clearance is predominantly extrahepatic.
[(1S,2S,5R)-5-methyl-2-propan-2-ylcyclohexyl]-phenylphosphoryl]benzene is a chemical compound that has gained significant attention in scientific research due to its potential therapeutic and environmental applications. This paper aims to provide an overview of the synthesis, chemical structure, biological activity, and potential applications of this compound.
Potent and selective, nonpeptide CCK2 receptor antagonist (IC50 values are 2.8 and 1232 nM for CCK2 and CCK1 respectively) that displays negligible affinity at GABAA, benzodiazepine, substance P, neurotensin, opioid, bradykinin and 5-HT3 receptors (IC50 > 10 μM). Exhibits anxiolytic activity in elevated plus maze and social interaction tests and increases food intake in rats.
Benzenamine, 2,6-diethyl-N-2-imidazolidinylidene-, monohydrochloride, also known as imazalil, is a fungicide that is commonly used in agriculture and horticulture to protect crops from fungal infections. It is also used in the food industry to prevent the growth of mold on fruits and vegetables during storage and transportation. Imazalil is a white crystalline powder that is soluble in water and organic solvents.
L-368,899 hydrochloride is a synthetic compound that belongs to the class of non-peptide oxytocin receptor antagonists. It has been extensively studied for its potential therapeutic applications in various medical conditions, including autism, anxiety, and schizophrenia.
CL 82198 hydrochloride is a synthetic compound that belongs to the class of benzodiazepines. It is a potent and selective agonist of the GABA-A receptor, which is responsible for the regulation of inhibitory neurotransmission in the central nervous system. CL 82198 hydrochloride has been extensively studied for its potential therapeutic applications in various medical conditions, including anxiety, insomnia, and epilepsy.
EGFR (epidermal growth factor receptor), ErbB-2, and ErbB-4 are members of the ErbB family of receptor tyrosine kinases. These receptors play a crucial role in cell growth, differentiation, and survival. Overexpression or mutation of these receptors has been linked to the development and progression of various cancers. Therefore, inhibitors of these receptors have been developed as potential anticancer agents.
High affinity σ1 receptor ligand that displays selectivity over σ2 receptors (Ki values are 10 and 370 nM respectively). Exhibits low affinity for dopamine (DAT), serotonin (SERT) and noradrenalin (NET) transporters (Ki > 10 μM) and low affinity for dopamine D2 receptors (Ki = 1226 nM). Attenuates cocaine-induced locomotor activity in mice.