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A P2X purinoceptor cDNA conferring a novel pharmacological profile
Abstract
We have cloned P2X 4, a member of the P2‐purinoceptor family, which has a new pharmacological profile. Rat P2X 4 is distantly related to P2X 1, P2X 2 and P2X 3 and is expressed in brain, spinal cord, lung, thymus, bladder, adrenal, testis and vas deferens. This ligand gated ion channel is activated by ATP and analogs with the potency order of ATP > ATP γ S > 2‐methylthio ATP > ADP ≈ αβ‐methylene ATP. However, none of the currently used P2X purinoceptor antagonists suramin, reactive blue 2 and PPADS blocked ATP evoked currents; in contrast their application resulted in potentiation of the agonist response. Due to lack of any known antagonist for P2X 4 it is unlikely that native P2X 4 has previously been recognized as a P2X purinoceptor.
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Citations
Cited by
Molecular Physiology of P2X Receptors
North, R. A. (2002) · Physiological Reviews · doi:10.1152/physrev.00015.2002 · Cited by 2,919
Allosteric Control of Gating and Kinetics at P2X4Receptor Channels
Khakh, B. S., Proctor, W. R., Dunwiddie, T. V., Labarca, C., & Lester, H. A. (1999) · The Journal of Neuroscience · doi:10.1523/jneurosci.19-17-07289.1999 · Cited by 279
Purinergic regulation of cholangiocyte secretion: identification of a novel role for P2X receptors
Doctor, R. B., Matzakos, T., McWilliams, R., Johnson, S., Feranchak, A. P., & Fitz, J. G. (2005) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.00325.2004 · Cited by 71
Metadata
- Authors
- Bo, X., Zhang, Y., Nassar, M., Burnstock, G., & Schoepfer, R.
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 1995-11-13
- Volume
- 375
- Issue
- 1-2
- Pages
- 129-133
- ISSN
- 0014-5793 (ISSN-L)
- 1873-3468
- OpenAlex
- W1968123967
- Cited by
- 278
- References
- 0
- FWCI
- 15.23
- Type
- journal article
- Language
- en
- Open access
- closed
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- Bo, X., Zhang, Y., Nassar, M., Burnstock, G., & Schoepfer, R. (1995). A P2X purinoceptor cDNA conferring a novel pharmacological profile. FEBS Letters. https://doi.org/10.1016/0014-5793(95)01203-q
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.