Title : The novel pyridoxal-5'-phosphate derivative PPNDS potently antagonizes activation of P2X(1) receptors - Lambrecht_2000_Eur.J.Pharmacol_387_R19 |
Author(s) : Lambrecht G , Rettinger J , Baumert HG , Czeche S , Damer S , Ganso M , Hildebrandt C , Niebel B , Spatz-Kumbel G , Schmalzing G , Mutschler E |
Ref : European Journal of Pharmacology , 387 :R19 , 2000 |
Abstract :
Pyridoxal-5'-phosphate-6-(2'-naphthylazo-6'-nitro-4',8'-disulfonat e) (PPNDS) potently antagonized P2X(1) receptor-mediated responses in rat vas deferens (pK(B)=7.43) and Xenopus laevis oocytes (pIC(50)=7. 84). It showed lower (up to 20,000-fold) inhibitory potency on ecto-nucleotidase in Xenopus oocytes and on P2Y(1) receptors in guinea-pig ileum (pA(2)=6.13). PPNDS did not interact with alpha(1A)-adrenoceptors, adenosine A(1) and A(2B), histamine H(1) and muscarinic M(3) receptors. Thus, PPNDS is a novel, specific P2 receptor antagonist and represents the pyridoxal-5'-phosphate derivative with the highest potency at P2X(1) receptors. |
PubMedSearch : Lambrecht_2000_Eur.J.Pharmacol_387_R19 |
PubMedID: 10650184 |
Lambrecht G, Rettinger J, Baumert HG, Czeche S, Damer S, Ganso M, Hildebrandt C, Niebel B, Spatz-Kumbel G, Schmalzing G, Mutschler E (2000)
The novel pyridoxal-5'-phosphate derivative PPNDS potently antagonizes activation of P2X(1) receptors
European Journal of Pharmacology
387 :R19
Lambrecht G, Rettinger J, Baumert HG, Czeche S, Damer S, Ganso M, Hildebrandt C, Niebel B, Spatz-Kumbel G, Schmalzing G, Mutschler E (2000)
European Journal of Pharmacology
387 :R19