The suramin analog 4,4′,4″,4‴-(carbonylbis(imino-5,1,3- benzenetriylbis (carbonylimino)))tetra-kis-benzenesulfonic acid (NF110) potently blocks P2X3 receptors: Subtype selectivity is determined by location of sulfonic acid groups

Molecular Pharmacology

Volumn 69, Issue 6, 2006, Pages 2058-2067

  Hausmann, Ralf ^a   Rettinger, Jürgen ^b   Gerevich, Zoltan ^c   Meis, Sabine ^d   Kassack, Matthias U ^d   Illes, Peter ^c   Lambrecht, Günter ^e   Schmalzing, G̈unther ^a,f  

^a RWTH AACHEN UNIVERSITY   (Germany)

^b MAX PLANCK INSTITUTE OF BIOPHYSICS   (Germany)

^c UNIVERSITY OF LEIPZIG   (Germany)

^d UNIVERSITY OF BONN   (Germany)

^e GOETHE UNIVERSITY   (Germany)

^f UNIVERSITY HOSPITAL RWTH AACHEN   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

2 (2,2',2'',2''' (CARBONYLBIS(IMINO 5,1,3 BENZENETRIYLBIS (CARBONYLIMINO)))TETRA KIS BENZENESULFONIC ACID; 3 (3,3',3'',3''' (CARBONYL BIS(IMINO 5,1,3 BENEZENETRIYLBIS (CARBONYLIMINO)))TETRA KIS BENZENESULFONIC ACID; 4 4,4'4'',4''' (CARBONYLBIS(IMINO 5,1,3 BENZENETRIYLBIS (CARBONYLIMINO)))TETRA KIS BENEZENESULFONIC ACID; ADENOSINE TRIPHOSPHATE; ALPHA BETA METHYLENE ADENOSINE TRIPHOSPHATE; AMIDE; BENZENE; MK 3; NF 110; NF 448; NF 449; PURINE P2X3 RECEPTOR; PURINERGIC RECEPTOR BLOCKING AGENT; SULFONIC ACID DERIVATIVE; SURAMIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG INHIBITION; DRUG MECHANISM; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; ELECTRODE; ELECTROPHYSIOLOGY; MALE; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; PRIORITY JOURNAL; RAT; SPINAL GANGLION; XENOPUS LAEVIS;

ADENOSINE TRIPHOSPHATE; ANIMALS; BENZENESULFONATES; OOCYTES; PATCH-CLAMP TECHNIQUES; PHENYLUREA COMPOUNDS; RATS; RECEPTORS, PURINERGIC P2; SULFONIC ACIDS; SURAMIN; XENOPUS LAEVIS;

EID: 33745146902     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.106.022665     Document Type: Article

References (40)

1. 1+2 receptor subtypes. J Mol Biol 342:333-343.
2. 3 receptor subunit in rat sensory neurons reveals a significant role in chronic neuropathic and inflammatory pain. J Neurosci 22:8139-8147.
3. 2/3 receptors by 2′,3′-O-(2,4,6-trinitrophenyl) adenosine 5′-triphosphate (TNP-ATP). Mol Pharmacol 58:1502-1510.
4. Burnstock G (2006) Purinergic P2 receptors as targets for novel analgesics. Pharmacol Ther, in press.
5. 50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
6. Chizh BA and Illes P (2001) P2X receptors and nociception. Pharmacol Rev 53:553-568.
7. 3-deficient mice. Nature (Lond) 407:1011-1015.
8. 6 receptors and the distribution and properties of an extended family of ATP-gated ion channels. J Neurosci 16:2495-2507.
9. Dorn G, Patel S, Wotherspoon G, Hemmings-Mieszczak M, Barclay J, Natt FJ, Martin P, Bevan S, Fox A, Ganju P, et al. (2004) siRNA relieves chronic neuropathic pain. Nucleic Acids Res 32:e49.
10. Driessen B, Reimann W, Selve N, Friderichs E, and Bültmann R (1994) Antinociceptive effect of intrathecally administered P2 purinoceptor antagonists in rats. Brain Res 666:182-188.
11. Egan TM, Cox JA, and Voigt MM (2004) Molecular structure of P2X receptors. Curr Top Med Chem 4:821-829.
12. 1 receptors. J Biol Chem 275:29361-29367.
13. Gerevich Z, Muller C, and Illes P (2005) Metabotropic P2Y(1) receptors inhibit P2X(3) receptor-channels in rat dorsal root ganglion neurons. Eur J Pharmacol 521:34-38.
14. 2 receptor desensitization depends on coupling between ectodomain and C-terminal domain. Mol Pharmacol 62:1187-1197.
15. 3 receptor antagonist, blocks acetic acid-induced abdominal constriction in mice: comparison with reference analgesics. Pain 96:99-105.
16. 1 receptors in human platelets with potency in the low nanomolar range. Naunyn-Schmiedeberg's Arch Pharmacol 372:1-13.
17. 1 receptors. Eur J Pharmacol 470:1-7.
18. Jacobson KA, Costanzi S, Ohno M, Joshi BV, Besada P, Xu B, and Tchilibon S (2004) Molecular recognition at purine and pyrimidine nucleotide (P2) receptors. Curr Top Med Chem 4:805-819.
19. 2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Proc Natl Acad Sci USA 99:17179-17184.
20. Jiang LH, Rassendren F, Surprenant A, and North RA (2000) Identification of amino acid residues contributing to the ATP-binding site of a purinergic P2X receptor. J Biol Chem 275:34190-34196.
21. 1 receptor antagonist. Eur J Med Chem 39:345-357.
22. Kennedy C (2005) P2X receptors: targets for novel analgesics? Neuroscientist 11: 345-356.
23. Khakh BS, Burnstock G, Kennedy C, King BF, North RA, Seguela P, Voigt M, and Humphrey PP (2001) International union of pharmacology. XXIV. Current status of the nomenclature and properties of P2X receptors and their subunits. Pharmacol Rev 53:107-118.
24. Lambrecht G, Braun K, Damer M, Ganso M, Hildebrandt C, Ullmann H, Kassack MU, and Nickel P (2002) Structure-activity relationships of suramin and pyridoxal-5′-phosphate derivatives as P2 receptor antagonists. Curr Pharm Des 8:2371-2399.
25. 3 receptor subunits can account for ATP-gated currents in sensory neurons. Nature (Lond) 377:432-435.
26. 2 receptor subunits in varying amounts generates heterogeneous populations of P2X receptors that evoke a spectrum of agonist responses comparable with that seen in sensory neurons. J Pharmacol Exp Ther 296:1043-1050.
27. 2/3 receptor antagonist, on neuropathic, inflammatory and chemogenic nociception following intrathecal and intraplantar administration. Br J Pharmacol 140:1381-1388.
28. 2 receptor with a crown-capped extracellular domain. Biochem Biophys Res Commun 337:998-1005.
29. 3 receptor. Br J Pharmacol 140:202-210.
30. 3 receptors form stable trimers: a novel structural motif of ligand-gated ion channels. EMBO (Eur Mol Biol Organ) J 17:3016-3028.
31. North RA (2002) Molecular physiology of P2X receptors. Physiol Rev 82:1013-1067.
32. 3 receptors and peripheral pain mechanisms. J Physiol (Lond) 554:301-308.
33. 3-receptors present in neurones of the rat dorsal root ganglia. Br J Pharmacol 124:176-180.
34. 1 receptor antagonist. Neuropharmacology 48:461-468.
35. 1 receptor. J Biol Chem 279:6426-6433.
36. 1 receptor. Neuropharmacology 39:2044-2053.
37. 3 receptors. Nature (Lond) 407:1015-1017.
38. 11 receptor antagonists with nanomolar potency. J Med Chem 48:7040-7048.
39. 2/3 receptors. Mol Pharmacol 53:969-973.
40. Werner P, Seward EP, Buell GN, and North RA (1996) Domains of P2X receptors involved in desensitization. Proc Natl Acad Sci USA 93:15485-15490.