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Characterization of the human cysteinyl leukotriene CysLT1 receptor
The molecular and pharmacological characterization of the cloned human CysLT1 receptor is reported and the functional activation (calcium mobilization) of this receptor is described by LTD4 and LTC4, and competition for radiolabelled LTD4 binding to this receptor by the cysteinyl leukotrienes and three structurally distinct classes of Cys LT1-receptor antagonists.
Characterization of the Human Cysteinyl Leukotriene 2 Receptor*
- C. Heise, B. O'dowd, Jilly F. Evans
- Biology, MedicineThe Journal of Biological Chemistry
- 29 September 2000
The cloning and characterization of the second cysteinyl leukotriene receptor, CysLT2, a 346-amino acid protein with 38% amino acid identity to the Cys LT1 receptor is described and demonstrated high affinity binding and a rank order of potency for competition of LTC4 = LTD4 ≫ LTE4.
Discovery of a receptor related to the galanin receptors
Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX‐2 inhibitor
The time‐dependent inhibition by DFU was decreased by co‐incubation with arachidonic acid under non‐turnover conditions, consistent with reversible competitive inhibition at the COX active site.
Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2
Functional studies demonstrated that PGD2 activation of recombinant CRTH2 results in decrease of intracellular cAMP in a pertussis toxin‐sensitive manner and showed that CRTH 2 can functionally couple to the G‐protein Gαi/o.
Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles.
- C. Chan, S. Boyce, I. Rodger
- Biology, MedicineThe Journal of pharmacology and experimental…
- 1 August 1999
Rofecoxib is a novel COX-2 inhibitor with a biochemical and pharmacological profile clearly distinct from that of current nonsteroidal anti-inflammatory drugs and represents a new therapeutic class of anti- inflammatory agents for the treatment of the symptoms of osteoarthritis and rheumatoid arthritis with improved gastrointestinal tolerability.
Selective modulation of chemokinesis, degranulation, and apoptosis in eosinophils through the PGD2 receptors CRTH2 and DP.
- F. Gervais, R. P. Cruz, G. O'neill
- Biology, MedicineThe Journal of allergy and clinical immunology
- 1 December 2001
These data support the hypothesis that PGD(2) controls eosinophil functions through 2 pharmacologically distinct receptors with independent functions and suggest a role for CRTH2 in the modulation of eos inophil movement and in triggering the release of cytotoxic proteins.
Expression of mRNA for cyclooxygenase‐1 and cyclooxygenase‐2 in human tissues
Identification of a GABAB Receptor Subunit, gb2, Required for Functional GABAB Receptor Activity*
Characterization of the tissue distribution of each of the receptors by in situhybridization histochemistry in rat brain revealed co-localization of gb1 and gb2 transcripts in many brain regions, suggesting the hypothesis that gb 1 and gB2 may interact in vivo.
Molecular Characterization and Expression of Cloned Human Galanin Receptors GALR2 and GALR3
The cloning of the human GALR2 and GALr3 genes is reported, an initial characterization of their pharmacology with respect to radioligand binding and signal transduction pathways, and a profile of their expression in brain and peripheral tissues is reported.