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Diinosine pentaphosphate: an antagonist which discriminates between recombinant P2X(3) and P2X(2/3) receptors and between two P2X receptors in rat sensory neurones.
Br J Pharmacol 2000; 130(6):1378-84BJ

Abstract

1. We have compared the antagonist activity of trinitrophenyl-ATP (TNP-ATP) and diinosine pentaphosphate (Ip(5)I) on recombinant P2X receptors expressed in Xenopus oocytes with their actions at native P2X receptors in sensory neurones from dorsal root and nodose ganglia. 2. Slowly-desensitizing responses to alpha,beta-methylene ATP (alpha,beta-meATP) recorded from oocytes expressing P2X(2/3) receptors were inhibited by TNP-ATP at sub-micromolar concentrations. However, Ip(5)I at concentrations up to 30 microM was without effect. 3. Nodose ganglion neurones responded to alpha,beta-meATP with slowly-desensitizing inward currents. These were inhibited by TNP-ATP (IC(50), 20 nM), but not by Ip(5)I at concentrations up to 30 microM. 4. In DRG neurones that responded to ATP with a rapidly-desensitizing inward current, the response was inhibited by TNP-ATP with an IC(50) of 0.8 nM. These responses were also inhibited by Ip(5)I with an IC(50) of 0.1 microM. Both antagonists are known to inhibit homomeric P2X(3) receptors. 5. Some DRG neurones responded to alpha,beta-meATP with a biphasic inward current, consisting of transient and sustained components. While the transient current was abolished by 1 microM Ip(5)I, the sustained component remained unaffected. 6. In conclusion, Ip(5)I is a potent antagonist at homomeric P2X(3) receptors but not at heteromeric P2X(2/3) receptors, and therefore should be a useful tool for elucidating the subunit composition of native P2X receptors.

Authors+Show Affiliations

Autonomic Neuroscience Institute, Royal Free and University College Medical School, London. p.dunn@ucl.ac.ukNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

10903979

Citation

Dunn, P M., et al. "Diinosine Pentaphosphate: an Antagonist Which Discriminates Between Recombinant P2X(3) and P2X(2/3) Receptors and Between Two P2X Receptors in Rat Sensory Neurones." British Journal of Pharmacology, vol. 130, no. 6, 2000, pp. 1378-84.
Dunn PM, Liu M, Zhong Y, et al. Diinosine pentaphosphate: an antagonist which discriminates between recombinant P2X(3) and P2X(2/3) receptors and between two P2X receptors in rat sensory neurones. Br J Pharmacol. 2000;130(6):1378-84.
Dunn, P. M., Liu, M., Zhong, Y., King, B. F., & Burnstock, G. (2000). Diinosine pentaphosphate: an antagonist which discriminates between recombinant P2X(3) and P2X(2/3) receptors and between two P2X receptors in rat sensory neurones. British Journal of Pharmacology, 130(6), pp. 1378-84.
Dunn PM, et al. Diinosine Pentaphosphate: an Antagonist Which Discriminates Between Recombinant P2X(3) and P2X(2/3) Receptors and Between Two P2X Receptors in Rat Sensory Neurones. Br J Pharmacol. 2000;130(6):1378-84. PubMed PMID: 10903979.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Diinosine pentaphosphate: an antagonist which discriminates between recombinant P2X(3) and P2X(2/3) receptors and between two P2X receptors in rat sensory neurones. AU - Dunn,P M, AU - Liu,M, AU - Zhong,Y, AU - King,B F, AU - Burnstock,G, PY - 2000/7/25/pubmed PY - 2000/9/19/medline PY - 2000/7/25/entrez SP - 1378 EP - 84 JF - British journal of pharmacology JO - Br. J. Pharmacol. VL - 130 IS - 6 N2 - 1. We have compared the antagonist activity of trinitrophenyl-ATP (TNP-ATP) and diinosine pentaphosphate (Ip(5)I) on recombinant P2X receptors expressed in Xenopus oocytes with their actions at native P2X receptors in sensory neurones from dorsal root and nodose ganglia. 2. Slowly-desensitizing responses to alpha,beta-methylene ATP (alpha,beta-meATP) recorded from oocytes expressing P2X(2/3) receptors were inhibited by TNP-ATP at sub-micromolar concentrations. However, Ip(5)I at concentrations up to 30 microM was without effect. 3. Nodose ganglion neurones responded to alpha,beta-meATP with slowly-desensitizing inward currents. These were inhibited by TNP-ATP (IC(50), 20 nM), but not by Ip(5)I at concentrations up to 30 microM. 4. In DRG neurones that responded to ATP with a rapidly-desensitizing inward current, the response was inhibited by TNP-ATP with an IC(50) of 0.8 nM. These responses were also inhibited by Ip(5)I with an IC(50) of 0.1 microM. Both antagonists are known to inhibit homomeric P2X(3) receptors. 5. Some DRG neurones responded to alpha,beta-meATP with a biphasic inward current, consisting of transient and sustained components. While the transient current was abolished by 1 microM Ip(5)I, the sustained component remained unaffected. 6. In conclusion, Ip(5)I is a potent antagonist at homomeric P2X(3) receptors but not at heteromeric P2X(2/3) receptors, and therefore should be a useful tool for elucidating the subunit composition of native P2X receptors. SN - 0007-1188 UR - https://www.unboundmedicine.com/medline/citation/10903979/Diinosine_pentaphosphate:_an_antagonist_which_discriminates_between_recombinant_P2X_3__and_P2X_2/3__receptors_and_between_two_P2X_receptors_in_rat_sensory_neurones_ L2 - https://doi.org/10.1038/sj.bjp.0703404 DB - PRIME DP - Unbound Medicine ER -