نتایج جستجو برای: relative potency
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In many animal species, as well as in humans, high doses of fentanyl (F) produce marked neurotoxic effects, such as muscular rigidity and respiratory depression. The antinociception (hot-plate test), impairment of motor coordination (rotarod test) and acute toxicity of intraperitoneal newly synthesized analogs, (±)cis-3-carbomethoxyfentanyl (C) and (±)trans-3-carbomethoxyfentanyl (T) were evalu...
The concurrent implementation of a proteome-wide serine hydrolase selectivity screen with traditional efforts to optimize fatty acid amide hydrolase (FAAH) inhibition potency led to the expedited discovery of a new class of exceptionally potent (Ki < 300 pM) and unusually selective (> 100-fold selective) inhibitors. The iterative inhibitor design and evaluation with assistance of the selectivit...
An in vitro bioassay for cholecystokinin which is superior to the previously described in vivo assays has been properly validated mathematically. The specificity of the assay has been assessed by measuring the potency of other polypeptides which share the same C-terminal pentapeptide sequence with cholecystokinin (gastrin, caerulin, octapeptide of cholecystokinin, and pentagastrin). The assay i...
Cholera toxin (CT), the causative agent of cholera, displays a pentavalent binding domain that targets the oligosaccharide of ganglioside GM1 (GM1os) on the periphery of human abdominal epithelial cells. Here, we report the first GM1os-based CT inhibitor that matches the valency of the CT binding domain (CTB). This pentavalent inhibitor contains five GM1os moieties linked to a calix[5]arene sca...
A growing subset of β-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease (AD) utilizes an anilide chemotype that engages a key residue (Gly230) in the BACE1 binding site. Although the anilide moiety affords excellent potency, it simultaneously introduces a third hydrogen bond donor that limits brain availability and provides a potential metabolic site leading to the formation...
S U M M A R Y We decompose a general seismic potency tensor into isotropic tensor, double-couple tensor and compensated linear vector dipole using the eigenvectors and eigenvalues of the full tensor. Two dimensionless parameters are used to quantify the size of the isotropic and compensated linear vector dipole components. The parameters have well-defined finite ranges and are suited for non-li...
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