NF449, a novel picomolar potency antagonist at human P2X1 receptors

European Journal of Pharmacology

Volumn 470, Issue 1-2, 2003, Pages 1-7

  Hülsmann, Martin ^a   Nickel, Peter ^b   Kassack, Matthias ^b   Schmalzing, Günther ^c   Lambrecht, Günter ^d   Markwardt, Fritz ^a  

^a MARTIN LUTHER UNIVERSITY HALLE WITTENBERG   (Germany)

^b UNIVERSITY OF BONN   (Germany)

^c RWTH AACHEN UNIVERSITY   (Germany)

^d GOETHE UNIVERSITY   (Germany)

Author keywords

Antagonist; ATP receptor; NF449 (4,4 ,4 ,4 (carbonylbis(imino 5,1,3 benzenetriylbis(carbonylimino)))tetrakis benzene 1,3 disulfonic acid); Oocyte; Voltage clamp; Whole cell

Indexed keywords

4,4',4'',4'' [CARBONYLBIS[IMINO 5,1,3 BENZENETRIYLBIS(CARBONYLIMINO)]]TETRAKIS BENZENE 1,3 DISULFONIC ACID; NF 449; PURINE P2X RECEPTOR; SULFONIC ACID DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG EFFECT; DRUG INFORMATION; DRUG MECHANISM; DRUG POTENCY; DRUG SELECTIVITY; HUMAN; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; VOLTAGE CLAMP; XENOPUS;

EID: 0038022869     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(03)01761-8     Document Type: Article

References (29)

1. Adrian K., Bernhard M.K., Breitinger H.G., Ogilvie A. Expression of purinergic receptors (ionotropic P2X1-7 and metabotropic P2Y1-11) during myeloid differentiation of HL60 cells. Biochim. Biophys. Acta. 1492:2000;127-138.
2. 1 receptors. Naunyn-Schmiedeberg's Arch. Pharmacol. 364:2001;285-290.
3. Bretschneider F., Markwardt F. Drug-dependent ion channel gating by application of concentration jumps using U-tube technique. Methods Enzymol. 294:1999;180-189.
4. 1/2 receptors show a novel sensitivity to extracellular pH. J. Pharmacol. Exp. Ther. 300:2002;673-680.
5. Damer S., Niebel B., Czeche S., Nickel P., Ardanuy U., Schmalzing G., Rettinger J., Mutschler E., Lambrecht G. NF279: a novel potent and selective antagonist of P2X receptor-mediated responses. Eur. J. Pharmacol. 350:1998;5-6.
6. Di Virgilio F. The P2Z purinoceptor: an intriguing role in immunity, inflammation and cell death. Immunol. Today. 16:1995;524-528.
7. Hohenegger M., Waldhoer M., Beindl W., Boing B., Kreimeyer A., Nickel P., Nanoff C., Freissmuth M. Gs-selective G protein antagonists. Proc. Natl. Acad. Sci. U. S. A. 95:1998;346-351.
8. 7 containing purinergic receptors in Müller cells of the rat retina. Mol. Brain Res. 76:2000;205-210.
9. Jacobson K.A., Jarvis M.F., Williams M. Purine and pyrimidine (P2) receptors as drug targets. J. Med. Chem. 45:2002;4057-4093.
10. Khakh B.S., Burnstock G., Kennedy C., King B.F., North R.A., Seguela P., Voigt M., Humphrey P.P.A. International union of pharmacology: XXIV. Current status of the nomenclature and properties of P2X receptors and their subunits. Pharmacol. Rev. 53:2001;107-118.
11. 7 receptors from human B lymphocytes expressed in Xenopus oocytes. Biochim. Biophys. Acta. 1467:2000;444-456.
12. 7 receptors. Eur. J. Pharmacol. 387:2000;245-252.
13. 7 receptor. J. Physiol. (Lond.). 534:2001;25-35.
14. Lambrecht G. Agonists and antagonists acting at P2X receptors: selectivity profiles and functional implications. Naunyn-Schmiedeberg's Arch. Pharmacol. 362:2000;340-350.
15. Lambrecht G., Braun K., Damer S., Ganso M., Hildebrandt C., Ullmann H., Kassack M.U., Nickel P. Structure-activity relationships of suramin and pyridoxal-5′-phosphate derivatives as P2 receptor antagonists. Curr. Pharm. Des. 8:2002;2371-2399.
16. Lewis C.J., Evans R.J. P2X receptor immunoreactivity in different arteries from the femoral, pulmonary, cerebral, coronary and renal circulations. J. Vasc. Res. 38:2001;332-340.
17. 3 receptor subunits can account for ATP-gated currents in sensory neurons. Nature. 377:1995;432-435.
18. Liu M., King B.F., Dunn P.M., Rong W.F., Townsend-Nicholson A., Burnstock G. Coexpression of P2X3 and P2X2 receptor subunits in varying amounts generates heterogeneous populations of P2X receptors that evoke a spectrum of agonist responses comparable to that seen in sensory neurons. J. Pharmacol. Exp. Ther. 296:2001;1043-1050.
19. Markwardt F., Löhn M., Böhm M., Klapperstück M. Purinoceptor-operated cationic channels in human B lymphocytes. J. Physiol. (Lond.). 498:1997;143-151.
20. North R.A. Molecular physiology of P2X receptors. Physiol. Rev. 82:2002;1013-1067.
21. Nörenberg W., Illes P. Neuronal P2X receptors: localisation and functional properties. Naunyn-Schmiedeberg's Arch. Pharmacol. 362:2000;324-339.
22. Ralevic V., Burnstock G. Receptors for purines and pyrimidines. Pharmacol. Rev. 50:1998;413-492.
23. 7 - cloning and expression of a human cDNA. J. Biol. Chem. 272:1997;5482-5486.
24. 1 receptor. Neuropharmacology. 39:2000;2044-2053.
25. Schmalzing G., Gloor S., Omay H., Kroner S., Appelhans H., Schwarz W. Up-regulation of sodium pump activity in Xenopus laevis oocytes by expression of heterologous beta 1 subunits of the sodium pump. Biochem. J. 279:1991;329-336.
26. Soto F., Lambrecht G., Nickel P., Stühmer W., Busch A.E. Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptors. Neuropharmacology. 38:1999;141-149.
27. Torres G.E., Egan T.M., Voigt M.M. Hetero-oligomeric assembly of P2X receptor subunits - specificities exist with regard to possible partners. J. Biol. Chem. 274:1999;6653-6659.
28. - channels in Xenopus oocytes. Pflügers Arch. 429:1995;820-824.
29. Zhang Y., McBride D.W. Jr., Hamill O.P. The ion selectivity of a membrane conductance inactivated by extracellular calcium in Xenopus oocytes. J. Physiol. (Lond.). 508:1998;763-776.