Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Willem Soudijn"'
Publikováno v:
Medicinal Research Reviews. 25:398-426
It has been recently established that G-protein-coupled receptors (GPCRs) can be constitutively active, i.e., they can be active in the absence of an agonist. This activity can be inhibited by so-called inverse agonists. For a number of GPCRs, such i
Publikováno v:
Drug Discovery Today. 9:752-758
Allosteric modulation of G protein-coupled receptors has recently been recognized as an alternative approach to gain selectivity in drug action. In this overview, allosteric modulators that enhance or diminish the effects of (endogenous) agonists or
Publikováno v:
Current Topics in Medicinal Chemistry. 3:355-367
In this review the latest developments in ligand design for the adenosine A(1) receptor are summarized. Novel series of agonists and antagonists are discussed, leading to the conclusion that ligands truly selective for the human adenosine A(1) recept
Publikováno v:
British Journal of Pharmacology. 118:369-377
1. The purpose of the present study was to develop an experimental strategy for the quantification of the cardiovascular effects of non-selective adenosine receptor ligands at the adenosine A1 and A2a receptor in vivo. 2-Chloroadenosine (CADO) was us
Autor:
Adriaan P. IJzerman, Sarah L. Price, Willem Soudijn, Eleonora M. van der Wenden, Robert P. Apaya
Publikováno v:
Journal of Computer-Aided Molecular Design. 9:44-54
The electrostatic properties of adenosine-based agonists and xanthine-based antagonists for the adenosine A1 receptor were used to assess various proposals for their relative orientation in the unknown binding site. The electrostatic properties were
Autor:
Willem Soudijn, A. M. Van Rhee, M. van der Heijden, Margot W. Beukers, Peter Nickel, Adriaan P. IJzerman
Publikováno v:
European Journal of Pharmacology: Molecular Pharmacology. 268:1-7
Binding of the radioligand [35S]adenosine 5'-O-(2-thiodiphosphate) (ADP beta 35S) to P2 gamma purinoceptors on turkey erythrocyte membranes was used to determine the affinity of suramin and various suramin congeners belonging to different structure c
Synthesis and biological evaluation of lorglumide-like hybrid cholecystokinin-A receptor antagonists
Autor:
Ineke Van Wijngaarden, Willem Soudijn, Ingrid van den Brink, Arie van der Bent, Adriaan P. IJzerman
Publikováno v:
Drug Development Research. 31:197-205
The evaluation of gross structural homologies between the competitive cholecystokinin-A (CCK-A) receptor antagonists lorglumide and devazepide formerly enabled the development of compact hybrid analogues [Van der Bent et al. (1992): J Med Chem 35:104
Publikováno v:
European Journal of Pharmacology: Molecular Pharmacology. 266:57-62
In this study, we determined whether R75231, (+/-)-2-(aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-[5,5-bis( 4-fluoro- phenyl)pentyl]-1-piperazineacetamide, and its two enantiomers, all nucleoside transport inhibitors, could play a role as anti-ag
Autor:
Adriaan P. IJzerman, Willem Soudijn, Cornel J.M. Kerkhof, Irene M. Pirovano, Margot W. Beukers, Anton van Weert
Publikováno v:
Biochemical Pharmacology. 46:1959-1966
Ecto-ATPase (EC 3.6.1.15) is a plasma membrane-bound enzyme which degrades extracellular triphosphate nucleotides. Although its physiological function is still unclear, the enzyme obscures the study of P 2 purinoceptors (i.e. receptors for ATP and ot