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  • affinity
  • This is reflected in notable pharmacological differences, in particular, a 100-1000-fold-lower affinity of the rat A 3 AR for certain xanthine compounds compared with the recombinant human and sheep receptors ( 1 , 5-7 ). (aspetjournals.org)
  • compounds
  • This invention relates to pyrazole compounds that inhibit or modulate the activity of cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3), to the use of the compounds in the treatment or prophylaxis of disease states or conditions mediated by cyclin dependent kinases and glycogen synthase kinase-3, and to novel compounds having cyclin dependent kinase or glycogen synthase kinase-3 inhibitory or modulating activity. (allindianpatents.com)
  • regulation
  • Although several studies have detailed the mechanisms underlying agonist-mediated desensitization of the rat A 3 AR, the regulation of the human A 3 AR, which displays only a 70% amino acid identity with the rat homologue, has not been addressed. (aspetjournals.org)
  • We demonstrated previously that prolonged agonist exposure of CHO cells expressing a recombinant rat A 3 AR results in a desensitization of receptor function that is associated with the down-regulation of specific G protein subunits ( 9 ). (aspetjournals.org)
  • The purpose of this study was to examine the properties of TIPP at selected points of the signal transduction pathway (i.e., receptor binding, G-protein activation, and effector regulation) in GH 3 DORT cells (GH 3 cells expressing δ-opioid receptors) and compare them with that of an established δ-opioid agonist, [ d -Pen 2 , d -Pen 5 ]-enkephalin (DPDPE). (aspetjournals.org)
  • synthesis
  • Time course experiments revealed that the onset of sensitization was half-maximal between 2 and 3 hr but was not due to the synthesis of new proteins because cycloheximide treatment failed to inhibit sensitization. (aspetjournals.org)
  • formula
  • and in said formula (f2-0-3), R 51 and R 52 each independently represents a hydrogen atom, a lower alkyl group of 1 to 5 carbon atoms, a fluorine atom or a fluorinated lower alkyl group, m f and n f each independently represents an integer of 0 to 5 (provided that m f +n f ≧1), and q' represents an integer of 0 to (patentsencyclopedia.com)
  • 5. A negative resist composition according to claim 4, wherein said fluorine-containing resin component (F) comprises said structural unit (f1), and a structural unit (f2-1), which is represented by said general formula (f2-0), in which at least one of said R 1 to R 4 is an alkali-soluble group represented by said general formula (f2-0-1). (patentsencyclopedia.com)
  • activation
  • The inability of the sensitization process to alter the AC activity obtained in the presence of manganese chloride suggests that prolonged A 3 AR activation increases the coupling efficiency between G s and AC catalytic units. (aspetjournals.org)
  • these include cardioprotection and neuroprotection from prolonged ischemia, bronchoconstriction, mast cell and eosinophil activation, and induction of hypotension ( 1-3 ). (aspetjournals.org)
  • In assays measuring G-protein activation, TIPP failed to stimulate guanosine 5′- O -(3-[ 35 S]thio)triphosphate ([ 35 S]GTPγS) binding in membrane preparations, which is consistent with an antagonist profile. (aspetjournals.org)