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Autor:
J.-P. Gies, Yves Landry
Publikováno v:
Mini-Reviews in Medicinal Chemistry. 2:361-372
Heptahelical receptors are coupled to heterotrimeric GTP-binding proteins (G proteins) which transduce most signals through their alpha and betagamma subunits to effectors including adenylylcyclases, ion channels, phospholipases Cbeta, and phosphoino
Publikováno v:
Naunyn-Schmiedeberg's Archives of Pharmacology. 359:153-159
We investigated the effect of the glucocorticoid methylprednisolone on the modulation of the expression of the bradykinin B2 receptors in cultured, guinea-pig, tracheal, smooth muscle cells. These receptors are implicated in the pathogenesis of human
Publikováno v:
Fundamental & Clinical Pharmacology. 12:188-193
This study investigated the effect of the non-peptidic B 2 bradykinin (BK) receptor antagonist WIN 64338 on BK binding and BK-induced inositol phosphate formation on guinea-pig tracheal smooth muscle cells in culture. The presence of specific and sat
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:3025-3028
6-(4-Phenyl-benzyloxy-methyl) guvacine was synthesized. Surprisingly the compound was devoid of the γ-aminobutyric acid (GABA) uptake inhibitory activity of its parent compound guvacine, but instead showed affinities for the muscarinic M 1 and M 2 r
Publikováno v:
Journal of Receptors and Signal Transduction. 16:135-148
In this study we looked for evidence regarding a correlation between M2-muscarinic receptor binding affinity and ligand intrinsic activity. Guanine nucleotide-binding protein-coupled receptors have been shown to exist in both a high affinity and a lo
Publikováno v:
Pulmonary Pharmacology. 6:119-127
Summary: Muscarinic receptors present in guinea-pig lung were characterized using the M 3 selective radioligand [ 3 H]4-diphenylacetoxy-N-methyl-piperidine methiodide ([ 3 H]4-DAMP). In saturation studies, [ 3 H]4-DAMP identified two populations of b
Publikováno v:
American Journal of Physiology-Lung Cellular and Molecular Physiology. 264:L80-L86
Bombesin (Bn) and related agonists produce a potent contractile response in guinea pig peripheral airways in vitro, with the following relative potencies: bombesin > gastrin-releasing peptide (GRP) > neuromedin C ≫ neuromedin B. Specific GRP-prefer
Publikováno v:
ChemInform. 28
6-(4-Phenyl-benzyloxy-methyl) guvacine was synthesized. Surprisingly the compound was devoid of the γ-aminobutyric acid (GABA) uptake inhibitory activity of its parent compound guvacine, but instead showed affinities for the muscarinic M 1 and M 2 r
Publikováno v:
Current medicinal chemistry. 13(1)
Heptahelical receptors are coupled to heterotrimeric GTP-binding proteins (G-proteins) which transduce most signals through their alpha and betagamma subunits to effectors, enzymes and ion channels. Of the 367 heptahelical receptors for endogenous li