Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists
In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by applicatio...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Kulyk, V. B. [verfasserIn] Chyzhmakov, I. V. [verfasserIn] Volkova, T. M. [verfasserIn] Kryshtal, O. A. [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2015 |
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| Schlagwörter: |
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| Übergeordnetes Werk: |
Enthalten in: Neurophysiology - New York, NY [u.a.] : Consultants Bureau, 1969, 47(2015), 3 vom: Juni, Seite 185-190 |
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| Übergeordnetes Werk: |
volume:47 ; year:2015 ; number:3 ; month:06 ; pages:185-190 |
| Links: |
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| DOI / URN: |
10.1007/s11062-015-9519-9 |
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| Katalog-ID: |
SPR016215842 |
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| 520 | |a In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by application of an endogenous opioid, Leu-enkephalin (LEK); the above currents were evoked by application of α,β-Me-ATP. Under conditions of preliminary 2- to 4-min-long incubation of neurons with naloxone, 10 nM LEK completely blocked P2H3 currents (blocking developed within 2 min). Under control conditions (without incubation), the respective effect was observed only at much higher LEK concentrations (1 μM). Thus, the IC50 of inhibitory LEK action was reduced in this case from 10 nM to 1 nM. Naloxone in high concentrations (1 μM), when applied after the development of the LEK inhibitory effect, exerted a dissimilar influence on the amplitude of P2X3 currents. For a time (within 2-4 min), this amplitude exceeded the control values; later on, it returned to the initial value. Such ambivalent effect of the opioid peptide (LEK) is related to the fact that G-proteins, when binding to the ORs, can form complexes in two conformations, inhibitory (Gi/o) and stimulating (Gq/s). It is known that naloxone can increase the analgesic effect of morphine due to direct competitive antagonism with the Gq/s-bound conformation. Thus, ambivalent effects of opioids on P2X3 receptors are explained by an antagonist-induced shift of the equilibrium between conformations of G-protein complexes. | ||
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| 650 | 4 | |a opioid receptors |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a P2X3 receptors |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Leu-enkephalin (LEK) |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a naloxone |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Gi/o and Gq/s proteins |7 (dpeaa)DE-He213 | |
| 700 | 1 | |a Chyzhmakov, I. V. |e verfasserin |4 aut | |
| 700 | 1 | |a Volkova, T. M. |e verfasserin |4 aut | |
| 700 | 1 | |a Kryshtal, O. A. |e verfasserin |4 aut | |
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10.1007/s11062-015-9519-9 doi (DE-627)SPR016215842 (SPR)s11062-015-9519-9-e DE-627 ger DE-627 rakwb eng 610 ASE 44.90 bkl Kulyk, V. B. verfasserin aut Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists 2015 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by application of an endogenous opioid, Leu-enkephalin (LEK); the above currents were evoked by application of α,β-Me-ATP. Under conditions of preliminary 2- to 4-min-long incubation of neurons with naloxone, 10 nM LEK completely blocked P2H3 currents (blocking developed within 2 min). Under control conditions (without incubation), the respective effect was observed only at much higher LEK concentrations (1 μM). Thus, the IC50 of inhibitory LEK action was reduced in this case from 10 nM to 1 nM. Naloxone in high concentrations (1 μM), when applied after the development of the LEK inhibitory effect, exerted a dissimilar influence on the amplitude of P2X3 currents. For a time (within 2-4 min), this amplitude exceeded the control values; later on, it returned to the initial value. Such ambivalent effect of the opioid peptide (LEK) is related to the fact that G-proteins, when binding to the ORs, can form complexes in two conformations, inhibitory (Gi/o) and stimulating (Gq/s). It is known that naloxone can increase the analgesic effect of morphine due to direct competitive antagonism with the Gq/s-bound conformation. Thus, ambivalent effects of opioids on P2X3 receptors are explained by an antagonist-induced shift of the equilibrium between conformations of G-protein complexes. primary sensory neurons (dpeaa)DE-He213 opioid receptors (dpeaa)DE-He213 P2X3 receptors (dpeaa)DE-He213 Leu-enkephalin (LEK) (dpeaa)DE-He213 naloxone (dpeaa)DE-He213 Gi/o and Gq/s proteins (dpeaa)DE-He213 Chyzhmakov, I. V. verfasserin aut Volkova, T. M. verfasserin aut Kryshtal, O. A. verfasserin aut Enthalten in Neurophysiology New York, NY [u.a.] : Consultants Bureau, 1969 47(2015), 3 vom: Juni, Seite 185-190 (DE-627)325573433 (DE-600)2037679-0 1573-9007 nnns volume:47 year:2015 number:3 month:06 pages:185-190 https://dx.doi.org/10.1007/s11062-015-9519-9 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2070 GBV_ILN_2086 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2116 GBV_ILN_2118 GBV_ILN_2119 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 44.90 ASE AR 47 2015 3 06 185-190 |
| spelling |
10.1007/s11062-015-9519-9 doi (DE-627)SPR016215842 (SPR)s11062-015-9519-9-e DE-627 ger DE-627 rakwb eng 610 ASE 44.90 bkl Kulyk, V. B. verfasserin aut Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists 2015 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by application of an endogenous opioid, Leu-enkephalin (LEK); the above currents were evoked by application of α,β-Me-ATP. Under conditions of preliminary 2- to 4-min-long incubation of neurons with naloxone, 10 nM LEK completely blocked P2H3 currents (blocking developed within 2 min). Under control conditions (without incubation), the respective effect was observed only at much higher LEK concentrations (1 μM). Thus, the IC50 of inhibitory LEK action was reduced in this case from 10 nM to 1 nM. Naloxone in high concentrations (1 μM), when applied after the development of the LEK inhibitory effect, exerted a dissimilar influence on the amplitude of P2X3 currents. For a time (within 2-4 min), this amplitude exceeded the control values; later on, it returned to the initial value. Such ambivalent effect of the opioid peptide (LEK) is related to the fact that G-proteins, when binding to the ORs, can form complexes in two conformations, inhibitory (Gi/o) and stimulating (Gq/s). It is known that naloxone can increase the analgesic effect of morphine due to direct competitive antagonism with the Gq/s-bound conformation. Thus, ambivalent effects of opioids on P2X3 receptors are explained by an antagonist-induced shift of the equilibrium between conformations of G-protein complexes. primary sensory neurons (dpeaa)DE-He213 opioid receptors (dpeaa)DE-He213 P2X3 receptors (dpeaa)DE-He213 Leu-enkephalin (LEK) (dpeaa)DE-He213 naloxone (dpeaa)DE-He213 Gi/o and Gq/s proteins (dpeaa)DE-He213 Chyzhmakov, I. V. verfasserin aut Volkova, T. M. verfasserin aut Kryshtal, O. A. verfasserin aut Enthalten in Neurophysiology New York, NY [u.a.] : Consultants Bureau, 1969 47(2015), 3 vom: Juni, Seite 185-190 (DE-627)325573433 (DE-600)2037679-0 1573-9007 nnns volume:47 year:2015 number:3 month:06 pages:185-190 https://dx.doi.org/10.1007/s11062-015-9519-9 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2070 GBV_ILN_2086 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2116 GBV_ILN_2118 GBV_ILN_2119 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 44.90 ASE AR 47 2015 3 06 185-190 |
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10.1007/s11062-015-9519-9 doi (DE-627)SPR016215842 (SPR)s11062-015-9519-9-e DE-627 ger DE-627 rakwb eng 610 ASE 44.90 bkl Kulyk, V. B. verfasserin aut Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists 2015 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by application of an endogenous opioid, Leu-enkephalin (LEK); the above currents were evoked by application of α,β-Me-ATP. Under conditions of preliminary 2- to 4-min-long incubation of neurons with naloxone, 10 nM LEK completely blocked P2H3 currents (blocking developed within 2 min). Under control conditions (without incubation), the respective effect was observed only at much higher LEK concentrations (1 μM). Thus, the IC50 of inhibitory LEK action was reduced in this case from 10 nM to 1 nM. Naloxone in high concentrations (1 μM), when applied after the development of the LEK inhibitory effect, exerted a dissimilar influence on the amplitude of P2X3 currents. For a time (within 2-4 min), this amplitude exceeded the control values; later on, it returned to the initial value. Such ambivalent effect of the opioid peptide (LEK) is related to the fact that G-proteins, when binding to the ORs, can form complexes in two conformations, inhibitory (Gi/o) and stimulating (Gq/s). It is known that naloxone can increase the analgesic effect of morphine due to direct competitive antagonism with the Gq/s-bound conformation. Thus, ambivalent effects of opioids on P2X3 receptors are explained by an antagonist-induced shift of the equilibrium between conformations of G-protein complexes. primary sensory neurons (dpeaa)DE-He213 opioid receptors (dpeaa)DE-He213 P2X3 receptors (dpeaa)DE-He213 Leu-enkephalin (LEK) (dpeaa)DE-He213 naloxone (dpeaa)DE-He213 Gi/o and Gq/s proteins (dpeaa)DE-He213 Chyzhmakov, I. V. verfasserin aut Volkova, T. M. verfasserin aut Kryshtal, O. A. verfasserin aut Enthalten in Neurophysiology New York, NY [u.a.] : Consultants Bureau, 1969 47(2015), 3 vom: Juni, Seite 185-190 (DE-627)325573433 (DE-600)2037679-0 1573-9007 nnns volume:47 year:2015 number:3 month:06 pages:185-190 https://dx.doi.org/10.1007/s11062-015-9519-9 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2070 GBV_ILN_2086 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2116 GBV_ILN_2118 GBV_ILN_2119 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 44.90 ASE AR 47 2015 3 06 185-190 |
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10.1007/s11062-015-9519-9 doi (DE-627)SPR016215842 (SPR)s11062-015-9519-9-e DE-627 ger DE-627 rakwb eng 610 ASE 44.90 bkl Kulyk, V. B. verfasserin aut Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists 2015 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by application of an endogenous opioid, Leu-enkephalin (LEK); the above currents were evoked by application of α,β-Me-ATP. Under conditions of preliminary 2- to 4-min-long incubation of neurons with naloxone, 10 nM LEK completely blocked P2H3 currents (blocking developed within 2 min). Under control conditions (without incubation), the respective effect was observed only at much higher LEK concentrations (1 μM). Thus, the IC50 of inhibitory LEK action was reduced in this case from 10 nM to 1 nM. Naloxone in high concentrations (1 μM), when applied after the development of the LEK inhibitory effect, exerted a dissimilar influence on the amplitude of P2X3 currents. For a time (within 2-4 min), this amplitude exceeded the control values; later on, it returned to the initial value. Such ambivalent effect of the opioid peptide (LEK) is related to the fact that G-proteins, when binding to the ORs, can form complexes in two conformations, inhibitory (Gi/o) and stimulating (Gq/s). It is known that naloxone can increase the analgesic effect of morphine due to direct competitive antagonism with the Gq/s-bound conformation. Thus, ambivalent effects of opioids on P2X3 receptors are explained by an antagonist-induced shift of the equilibrium between conformations of G-protein complexes. primary sensory neurons (dpeaa)DE-He213 opioid receptors (dpeaa)DE-He213 P2X3 receptors (dpeaa)DE-He213 Leu-enkephalin (LEK) (dpeaa)DE-He213 naloxone (dpeaa)DE-He213 Gi/o and Gq/s proteins (dpeaa)DE-He213 Chyzhmakov, I. V. verfasserin aut Volkova, T. M. verfasserin aut Kryshtal, O. A. verfasserin aut Enthalten in Neurophysiology New York, NY [u.a.] : Consultants Bureau, 1969 47(2015), 3 vom: Juni, Seite 185-190 (DE-627)325573433 (DE-600)2037679-0 1573-9007 nnns volume:47 year:2015 number:3 month:06 pages:185-190 https://dx.doi.org/10.1007/s11062-015-9519-9 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2070 GBV_ILN_2086 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2116 GBV_ILN_2118 GBV_ILN_2119 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 44.90 ASE AR 47 2015 3 06 185-190 |
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10.1007/s11062-015-9519-9 doi (DE-627)SPR016215842 (SPR)s11062-015-9519-9-e DE-627 ger DE-627 rakwb eng 610 ASE 44.90 bkl Kulyk, V. B. verfasserin aut Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists 2015 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by application of an endogenous opioid, Leu-enkephalin (LEK); the above currents were evoked by application of α,β-Me-ATP. Under conditions of preliminary 2- to 4-min-long incubation of neurons with naloxone, 10 nM LEK completely blocked P2H3 currents (blocking developed within 2 min). Under control conditions (without incubation), the respective effect was observed only at much higher LEK concentrations (1 μM). Thus, the IC50 of inhibitory LEK action was reduced in this case from 10 nM to 1 nM. Naloxone in high concentrations (1 μM), when applied after the development of the LEK inhibitory effect, exerted a dissimilar influence on the amplitude of P2X3 currents. For a time (within 2-4 min), this amplitude exceeded the control values; later on, it returned to the initial value. Such ambivalent effect of the opioid peptide (LEK) is related to the fact that G-proteins, when binding to the ORs, can form complexes in two conformations, inhibitory (Gi/o) and stimulating (Gq/s). It is known that naloxone can increase the analgesic effect of morphine due to direct competitive antagonism with the Gq/s-bound conformation. Thus, ambivalent effects of opioids on P2X3 receptors are explained by an antagonist-induced shift of the equilibrium between conformations of G-protein complexes. primary sensory neurons (dpeaa)DE-He213 opioid receptors (dpeaa)DE-He213 P2X3 receptors (dpeaa)DE-He213 Leu-enkephalin (LEK) (dpeaa)DE-He213 naloxone (dpeaa)DE-He213 Gi/o and Gq/s proteins (dpeaa)DE-He213 Chyzhmakov, I. V. verfasserin aut Volkova, T. M. verfasserin aut Kryshtal, O. A. verfasserin aut Enthalten in Neurophysiology New York, NY [u.a.] : Consultants Bureau, 1969 47(2015), 3 vom: Juni, Seite 185-190 (DE-627)325573433 (DE-600)2037679-0 1573-9007 nnns volume:47 year:2015 number:3 month:06 pages:185-190 https://dx.doi.org/10.1007/s11062-015-9519-9 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2070 GBV_ILN_2086 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2116 GBV_ILN_2118 GBV_ILN_2119 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 44.90 ASE AR 47 2015 3 06 185-190 |
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Enthalten in Neurophysiology 47(2015), 3 vom: Juni, Seite 185-190 volume:47 year:2015 number:3 month:06 pages:185-190 |
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primary sensory neurons opioid receptors P2X3 receptors Leu-enkephalin (LEK) naloxone Gi/o and Gq/s proteins |
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Neurophysiology |
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Kulyk, V. B. @@aut@@ Chyzhmakov, I. V. @@aut@@ Volkova, T. M. @@aut@@ Kryshtal, O. A. @@aut@@ |
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2015-06-01T00:00:00Z |
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B.</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="245" ind1="1" ind2="0"><subfield code="a">Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists</subfield></datafield><datafield tag="264" ind1=" " ind2="1"><subfield code="c">2015</subfield></datafield><datafield tag="336" ind1=" " ind2=" "><subfield code="a">Text</subfield><subfield code="b">txt</subfield><subfield code="2">rdacontent</subfield></datafield><datafield tag="337" ind1=" " ind2=" "><subfield code="a">Computermedien</subfield><subfield code="b">c</subfield><subfield code="2">rdamedia</subfield></datafield><datafield tag="338" ind1=" " ind2=" "><subfield code="a">Online-Ressource</subfield><subfield code="b">cr</subfield><subfield code="2">rdacarrier</subfield></datafield><datafield tag="520" ind1=" " ind2=" "><subfield code="a">In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by application of an endogenous opioid, Leu-enkephalin (LEK); the above currents were evoked by application of α,β-Me-ATP. Under conditions of preliminary 2- to 4-min-long incubation of neurons with naloxone, 10 nM LEK completely blocked P2H3 currents (blocking developed within 2 min). Under control conditions (without incubation), the respective effect was observed only at much higher LEK concentrations (1 μM). Thus, the IC50 of inhibitory LEK action was reduced in this case from 10 nM to 1 nM. Naloxone in high concentrations (1 μM), when applied after the development of the LEK inhibitory effect, exerted a dissimilar influence on the amplitude of P2X3 currents. For a time (within 2-4 min), this amplitude exceeded the control values; later on, it returned to the initial value. Such ambivalent effect of the opioid peptide (LEK) is related to the fact that G-proteins, when binding to the ORs, can form complexes in two conformations, inhibitory (Gi/o) and stimulating (Gq/s). 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Kulyk, V. B. |
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Kulyk, V. B. ddc 610 bkl 44.90 misc primary sensory neurons misc opioid receptors misc P2X3 receptors misc Leu-enkephalin (LEK) misc naloxone misc Gi/o and Gq/s proteins Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists |
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610 ASE 44.90 bkl Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists primary sensory neurons (dpeaa)DE-He213 opioid receptors (dpeaa)DE-He213 P2X3 receptors (dpeaa)DE-He213 Leu-enkephalin (LEK) (dpeaa)DE-He213 naloxone (dpeaa)DE-He213 Gi/o and Gq/s proteins (dpeaa)DE-He213 |
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Kulyk, V. B. Chyzhmakov, I. V. Volkova, T. M. Kryshtal, O. A. |
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ambivalent effects on p2x3 receptors in rat sensory neurons in the presence of opioid receptor antagonists |
| title_auth |
Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists |
| abstract |
In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by application of an endogenous opioid, Leu-enkephalin (LEK); the above currents were evoked by application of α,β-Me-ATP. Under conditions of preliminary 2- to 4-min-long incubation of neurons with naloxone, 10 nM LEK completely blocked P2H3 currents (blocking developed within 2 min). Under control conditions (without incubation), the respective effect was observed only at much higher LEK concentrations (1 μM). Thus, the IC50 of inhibitory LEK action was reduced in this case from 10 nM to 1 nM. Naloxone in high concentrations (1 μM), when applied after the development of the LEK inhibitory effect, exerted a dissimilar influence on the amplitude of P2X3 currents. For a time (within 2-4 min), this amplitude exceeded the control values; later on, it returned to the initial value. Such ambivalent effect of the opioid peptide (LEK) is related to the fact that G-proteins, when binding to the ORs, can form complexes in two conformations, inhibitory (Gi/o) and stimulating (Gq/s). It is known that naloxone can increase the analgesic effect of morphine due to direct competitive antagonism with the Gq/s-bound conformation. Thus, ambivalent effects of opioids on P2X3 receptors are explained by an antagonist-induced shift of the equilibrium between conformations of G-protein complexes. |
| abstractGer |
In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by application of an endogenous opioid, Leu-enkephalin (LEK); the above currents were evoked by application of α,β-Me-ATP. Under conditions of preliminary 2- to 4-min-long incubation of neurons with naloxone, 10 nM LEK completely blocked P2H3 currents (blocking developed within 2 min). Under control conditions (without incubation), the respective effect was observed only at much higher LEK concentrations (1 μM). Thus, the IC50 of inhibitory LEK action was reduced in this case from 10 nM to 1 nM. Naloxone in high concentrations (1 μM), when applied after the development of the LEK inhibitory effect, exerted a dissimilar influence on the amplitude of P2X3 currents. For a time (within 2-4 min), this amplitude exceeded the control values; later on, it returned to the initial value. Such ambivalent effect of the opioid peptide (LEK) is related to the fact that G-proteins, when binding to the ORs, can form complexes in two conformations, inhibitory (Gi/o) and stimulating (Gq/s). It is known that naloxone can increase the analgesic effect of morphine due to direct competitive antagonism with the Gq/s-bound conformation. Thus, ambivalent effects of opioids on P2X3 receptors are explained by an antagonist-induced shift of the equilibrium between conformations of G-protein complexes. |
| abstract_unstemmed |
In cultured neurons of the dorsal root ganglia (DRGs) of rats, it was found that incubation of these neurons in the presence of 50 nM naloxone (an opioid receptor antagonist, OR antagonist) significantly increased the efficacy of blocking of P2X3-mediated transmembrane currents induced by application of an endogenous opioid, Leu-enkephalin (LEK); the above currents were evoked by application of α,β-Me-ATP. Under conditions of preliminary 2- to 4-min-long incubation of neurons with naloxone, 10 nM LEK completely blocked P2H3 currents (blocking developed within 2 min). Under control conditions (without incubation), the respective effect was observed only at much higher LEK concentrations (1 μM). Thus, the IC50 of inhibitory LEK action was reduced in this case from 10 nM to 1 nM. Naloxone in high concentrations (1 μM), when applied after the development of the LEK inhibitory effect, exerted a dissimilar influence on the amplitude of P2X3 currents. For a time (within 2-4 min), this amplitude exceeded the control values; later on, it returned to the initial value. Such ambivalent effect of the opioid peptide (LEK) is related to the fact that G-proteins, when binding to the ORs, can form complexes in two conformations, inhibitory (Gi/o) and stimulating (Gq/s). It is known that naloxone can increase the analgesic effect of morphine due to direct competitive antagonism with the Gq/s-bound conformation. Thus, ambivalent effects of opioids on P2X3 receptors are explained by an antagonist-induced shift of the equilibrium between conformations of G-protein complexes. |
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Ambivalent Effects on P2X3 Receptors in Rat Sensory Neurons in the Presence of Opioid Receptor Antagonists |
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Chyzhmakov, I. V. Volkova, T. M. Kryshtal, O. A. |
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| score |
7.4005556 |