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Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
- F. Dörje, J. Wess, G. Lambrecht, R. Tacke, E. Mutschler, M. Brann
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 February 1991
The affinity profiles of several of these antagonists at five cloned human muscarinic receptors stably expressed in Chinese hamster ovary cells are determined.
P2X1 and P2X3 receptors form stable trimers: a novel structural motif of ligand‐gated ion channels
It is concluded that trimers represent an essential element of P2X receptor structure and can aggregate to form larger complexes.
Agonists and antagonists acting at P2X receptors: selectivity profiles and functional implications
- G. Lambrecht
- BiologyNaunyn-Schmiedeberg's Archives of Pharmacology
- 19 August 2000
This work moves the field closer to the ideal goal of classifying the recombinant and native P2X receptor subtypes on the basis of antagonist profiles by identifying a series of key P2 receptor agonists and antagonists.
PPADS, a novel functionally selective antagonist of P2 purinoceptor-mediated responses.
Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptors
Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist
NF449: a subnanomolar potency antagonist at recombinant rat P2X1 receptors
- K. Braun, J. Rettinger, G. Lambrecht
- Biology, ChemistryNaunyn-Schmiedeberg's Archives of Pharmacology
- 1 September 2001
The subnanomolar potency at rP2X1 receptors and the rank order of potency, P 2X1 >> P2X3 > P 2Y1 > P2Y2 > ecto-nucleotidases, make NF449 unique among the P2 receptor antagonists reported to date.
NF449, a novel picomolar potency antagonist at human P2X1 receptors.
The suramin analogue NF279 is a novel and potent antagonist selective for the P2X1 receptor