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Evans blue blocks P2X-purinoceptors in rat vas deferens

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Summary

In rat vas deferens, Evans blue 100 μM increased contractions elicited by high K+ and by noradrenaline but markedly reduced contractions elicited by the P2X-purinoceptor-selective agonist α,β-methylene ATP (3 μM). The concentration-response curve of α,β-methylene ATP was shifted to the right by Evans blue 30 μM and the maximal contraction was increased. In tissues incubated with nifedipine 10 μM, Evans blue 100 μM tended to increase the residual contraction elicited by noradrenaline and abolished the residual response to α,β-methylene ATP (3 μM). The concentration-response curve of α,β-methylene ATP was progressively shifted to the right by increasing concentrations of Evans blue in the presence of nifedipine; maximal contractions were increased by Evans blue 10 and 30 but not 100 μM. From the shifts to the right caused by Evans blue 30 μM, apparent pKB values of 5.9 (no nifedipine) and 6.0 (nifedipine present) were calculated. It is concluded that Evans blue blocks P2X-purinoceptors in rat vas deferens and in addition causes a non-receptor-specific enhancement of contractions.

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References

  • Arunlakshana O, Schild HO (1959) Some quantitative uses of drug antagonists. Br J Pharmacol 14:48–58

    Google Scholar 

  • Bültmann R, Starke K (1994) P2-purinoceptor antagonists discriminate three contraction-mediating receptors for ATP in rat vas deferens. Naunyn-Schmiedebergs Arch Pharmacol 349: in press

  • Bültmann R, Szabo B, Starke K (1993) Inhibition by ethanol of contractions of rat vas deferens: no evidence for selective blockade of P2x-purinoceptors. Naunyn-Schmiedebergs Arch Pharmacol 347: 527–533

    Google Scholar 

  • Burnstock G, Kennedy C (1985) Is there a basis for distinguishing two types of P2-purinoceptor? Gen Pharmacol 16:433–440

    Google Scholar 

  • Burnstock G, Warland JJI (1987) P2-purinoceptors of two subtypes in the rabbit mesenteric artery: reactive blue 2 selectively inhibits responses mediated via the P2Y- but not the P2X-purinoceptor. Br J Pharmacol 90:383–391

    Google Scholar 

  • Cusack NJ (1993) P2 Receptor: subclassification and structure-activity relationships. Drug Dev Res 28:244–252

    Google Scholar 

  • Dunn PM, Blakeley AGH (1988) Suramin: a reversible P2-purinoceptor antagonist in the mouse vas deferens. Br J Pharmacol 93:243–245

    Google Scholar 

  • Furchgott RF (1972) The classification of adrenoceptors (adrenergic receptors). An evaluation from the standpoint of receptor theory. In: Blaschko H, Muscholl E (eds) Catecholamines. Handbook of experimental pharmacology, vol 33. Springer, Berlin Heidelberg New York, pp 283–335

    Google Scholar 

  • Huidobro Toro JP, Parada S (1988) Co-transmission in the rat vas deferens: postjunctional synergism of noradrenaline and adenosine 5′-triphosphate. Neurosci Lett 85:339–344

    Google Scholar 

  • Kennedy C (1990) P1- and P2-purinoceptor subtypes — an update. Arch Int Pharmacodyn 303:30–50

    Google Scholar 

  • Kerr DIB, Krantis A (1979) A new class of ATP antagonist. Proc Austr Physiol Pharmacol Soc 10:156P

    Google Scholar 

  • von Kügelgen I, Bültmann R, Starke K (1990) Interaction of adenine nucleotides, UTP and suramin in mouse vas deferens: suramin-sensitive and suramin-insensitive components in the contractile effect of ATP. Naunyn-Schmiedebergs Arch Pharmacol 342:198–205

    Google Scholar 

  • Lambrecht G, Friebe T, Grimm U, Windscheif U, Bungardt E, Hildebrandt C, Baumert HG, Spatz-Kümbel G, Mutschler E (1992) PPADS, a novel functionally selective antagonist of P2 purinoceptor-mediated responses. Eur J Pharmacol 217:217–219

    Google Scholar 

  • Mallard N, Marshall R, Sithers A, Spriggs B (1992) Suramin: a selective inhibitor of purinergic neurotransmission in the rat isolated vas deferens. Eur J Pharmacol 220:1–10

    Google Scholar 

  • McLaren GJ, Sneddon P, Kennedy C, Lambrecht G, Burnstock G, Mutschler E, Baumert HG, Hoyle CHV (1993) Investigation of a putative P2X-purinoceptor antagonist in guinea-pig isolated vas deferens. Br J Pharmacol 109:109P

  • Motulsky HJ, Ransnas LA (1987) Fitting curves to data using nonlinear regression: a practical and nonmathematical review. FASEB J 1:365–374

    Google Scholar 

  • Waud DR (1976) Analysis of dose-response relationships. In: Narahashi T, Bianchi CP (eds) Advances in general and cellular pharmacology, vol 1. Plenum, New York London, pp 145–178

    Google Scholar 

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Correspondence to: R. Bültmann at the above address

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Bültmann, R., Starke, K. Evans blue blocks P2X-purinoceptors in rat vas deferens. Naunyn-Schmiedeberg's Arch Pharmacol 348, 684–687 (1993). https://doi.org/10.1007/BF00167248

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  • DOI: https://doi.org/10.1007/BF00167248

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