Properties of the novel ATP-gated ionotropic receptor composed of the P2X1 and P2X5 isoforms
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Haines, WR
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St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USASt Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
Haines, WR
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Torres, GE
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St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USASt Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
Torres, GE
[1
]
Voigt, MM
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St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USASt Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
Voigt, MM
[1
]
Egan, TM
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St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USASt Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
Egan, TM
[1
]
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[1] St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
We recently reported that a novel hetero-oligomeric P2X receptor is formed from the P2X(1) and P2X(5) isoforms when coexpressed in human embryonic kidney 293 cells (Torres et al., 1998). A more complete description of the pharmacology of this novel receptor is presented here. A brief application of ATP to a voltage-clamped cell transiently expressing P2X(1/5) receptors resulted in a biphasic current that rapidly reached a peak and then decayed to a sustained plateau. Washout of ATP was accompanied by generation and fade of a pronounced tail of inward current. EC50 values were determined from concentration-response curves for a range of agonists. The rank order of agonist potency was ATP greater than or equal to 2 methylthio ATP > adenosine 5'-O-(3-thiotriphosphate) > alpha,beta-methylene ATP > ADP > CTP. alpha,beta-methylene ADP, UTP, GTP, and AMP were ineffective. Only ATP and 2 methylthio ATP were full agonists. IC50 values were determined from concentration-response curves for three commonly used purinergic antagonists. Suramin and pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid were equipotent at P2X(1) and P2X(1/5) receptors; however, the P2X(1/5) receptor was much less sensitive to TNP-ATP than was the P2X(1) receptor. The amplitude of peak ATP-gated current was relatively insensitive to changes in [Ca2+](o) (1-30 mM). Finally, plateau currents were potentiated by low concentrations of pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid and by raising [Ca2+](o). These results provide additional information on the pharmacological profile of the recombinant P2X(1/5) receptor channel and provide a basis to further evaluate ATP-induced currents in native tissues.
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Konkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Konkuk Univ, Bio Mol Informat Ctr, Seoul 143701, South KoreaKonkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Choi, Sun-Hye
Kim, Hyeon-Joong
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Konkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Konkuk Univ, Bio Mol Informat Ctr, Seoul 143701, South KoreaKonkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Kim, Hyeon-Joong
Kim, Bo-Ra
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Konkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Konkuk Univ, Bio Mol Informat Ctr, Seoul 143701, South KoreaKonkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Kim, Bo-Ra
Shin, Tae-Joon
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Konkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Konkuk Univ, Bio Mol Informat Ctr, Seoul 143701, South KoreaKonkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Shin, Tae-Joon
Hwang, Sung-Hee
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Konkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Konkuk Univ, Bio Mol Informat Ctr, Seoul 143701, South KoreaKonkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Hwang, Sung-Hee
Lee, Byung-Hwan
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Konkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Konkuk Univ, Bio Mol Informat Ctr, Seoul 143701, South KoreaKonkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Lee, Byung-Hwan
Lee, Sang-Mok
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Konkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Konkuk Univ, Bio Mol Informat Ctr, Seoul 143701, South KoreaKonkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
Lee, Sang-Mok
Rhim, Hyewhon
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Korea Inst Sci & Technol, Div Life Sci, Seoul 130701, South KoreaKonkuk Univ, Coll Vet Med, Dept Physiol, Seoul 143701, South Korea
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St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USASt Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
Torres, GE
Egan, TM
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St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USASt Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
Egan, TM
Voigt, MM
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St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USASt Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
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Cardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, SwedenCardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, Sweden
Grenegard, Magnus
Vretenbrant-Oberg, Karin
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Cardiovasc Inflammat Res Ctr, Div Clin Chem, Dept Clin & Expt Med, SE-58185 Linkoping, SwedenCardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, Sweden
Vretenbrant-Oberg, Karin
Nylander, Martina
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Cardiovasc Inflammat Res Ctr, Div Clin Chem, Dept Clin & Expt Med, SE-58185 Linkoping, SwedenCardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, Sweden
Nylander, Martina
Desilets, Stephanie
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Cardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, SwedenCardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, Sweden
Desilets, Stephanie
Lindstrom, Eva G.
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Cardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, SwedenCardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, Sweden
Lindstrom, Eva G.
Larsson, Anders
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Univ Uppsala Hosp, Dept Med Sci, SE-75105 Uppsala, SwedenCardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, Sweden
Larsson, Anders
Ramstrom, Ida
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Cardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, SwedenCardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, Sweden
Ramstrom, Ida
Ramstrom, Sofia
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Cardiovasc Inflammat Res Ctr, Div Clin Chem, Dept Clin & Expt Med, SE-58185 Linkoping, SwedenCardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, Sweden
Ramstrom, Sofia
Lindahl, Tomas L.
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Cardiovasc Inflammat Res Ctr, Div Clin Chem, Dept Clin & Expt Med, SE-58185 Linkoping, SwedenCardiovasc Inflammat Res Ctr, Div Drug Res, Dept Med & Hlth, SE-58185 Linkoping, Sweden
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St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USASt Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
Torres, GE
Egan, TM
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St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USASt Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
Egan, TM
Voigt, MM
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St Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USASt Louis Univ, Sch Med, Dept Pharmacol & Physiol Sci, St Louis, MO 63104 USA
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Glaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, SwitzerlandGlaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, Switzerland
Newbolt, A
Stoop, R
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Glaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, SwitzerlandGlaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, Switzerland
Stoop, R
Virginio, C
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Glaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, SwitzerlandGlaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, Switzerland
Virginio, C
Surprenant, A
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Glaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, SwitzerlandGlaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, Switzerland
Surprenant, A
North, RA
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Glaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, SwitzerlandGlaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, Switzerland
North, RA
Buell, G
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Glaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, SwitzerlandGlaxo Wellcome Res & Dev Ltd, Geneva Biomed Res Inst, CH-1228 Geneva, Switzerland
Buell, G
Rassendren, F
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