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Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
A variety of muscarinic antagonists are currently used as tools to pharmacologically subclassify muscarinic receptors into M1, M2 and M3 subtypes. In the present study, we have determined theExpand
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P2X1 and P2X3 receptors form stable trimers: a novel structural motif of ligand‐gated ion channels
P2X receptors are cation channels gated by extracellular ATP. The seven known P2X isoforms possess no sequence homology with other proteins. Here we studied the quaternary structure of P2X receptorsExpand
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PPADS, a novel functionally selective antagonist of P2 purinoceptor-mediated responses.
We have characterized PPADS (pyridoxalphosphate-6-azophenyl-2',4'-disulfonic acid) as a novel antagonist which selectively blocks P2 purinoceptor-mediated responses in rabbit vas deferens at pre- andExpand
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Agonists and antagonists acting at P2X receptors: selectivity profiles and functional implications
  • G. Lambrecht
  • Medicine, Chemistry
  • Naunyn-Schmiedeberg's Archives of Pharmacology
  • 19 August 2000
P2X receptors are nucleotide-gated cation channels composed of homomeric or heteromeric assemblies of three subunits. In the past 7 years, an extended series (P2X1–7) of P2X subunits has been clonedExpand
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Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptors
The suramin analogue 8,8'-(carbonylbis(imino-3,1-phenylene carbonylimino)bis(1,3,5-naphthalenetrisulfonic acid) (NF023) antagonizes in a competitive fashion P2X receptor-mediated responses in certainExpand
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Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist
P2X receptors are cation channels gated by extracellular ATP and related nucleotides. Because of the widespread distribution of P2X receptors and the high subtype diversity, potent and selectiveExpand
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NF449: a subnanomolar potency antagonist at recombinant rat P2X1 receptors
Abstract. Antagonistic effects of the novel suramin analogue 4,4′,4′′,4′′′-(carbonylbis(imino-5,1,3-benzenetriylbis(carbonylimino)))tetrakis-benzene-1,3-disulfonic acid (NF449) were studied onExpand
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The suramin analogue NF279 is a novel and potent antagonist selective for the P2X1 receptor
The suramin analogue 8,8'-(carbonylbis(imino-4, 1-phenylenecarbonylimino-4,1-phenylenecarbonylimino)) bis(1,3,5-naphthalenetrisul fonic acid) (NF279) was analysed with respect to its potency and P2XExpand
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NF449, a novel picomolar potency antagonist at human P2X1 receptors.
The antagonistic effects of the novel suramin analogue 4,4',4",4"'-(carbonylbis(imino-5,1,3-benzenetriylbis(carbonylimino)))tetrakis-benzene-1,3-disulfonic acid (NF449) were analyzed at homomericExpand
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Muscarinic receptors mediating acid secretion in isolated rat gastric parietal cells are of M3 type.
Five subtypes of muscarinic receptors have been identified by pharmacological and molecular biological methods. The muscarinic receptor subtype mediating acid secretion at the level of the parietalExpand
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