γ-Aminobutyric AcidA Receptor Pharmacology in Rat Cerebral Cortical Synaptoneurosomes
Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
DeLorey, Timothy M. [verfasserIn] Brown, George B. [verfasserIn] |
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| Format: |
E-Artikel |
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| Erschienen: |
Oxford, UK: Blackwell Publishing Ltd ; 1992 |
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| Schlagwörter: |
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| Umfang: |
Online-Ressource |
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| Reproduktion: |
2006 ; Blackwell Publishing Journal Backfiles 1879-2005 |
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| Übergeordnetes Werk: |
In: Journal of neurochemistry - Oxford : Wiley-Blackwell, 1956, 58(1992), 6, Seite 0 |
| Übergeordnetes Werk: |
volume:58 ; year:1992 ; number:6 ; pages:0 |
| Links: |
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| DOI / URN: |
10.1111/j.1471-4159.1992.tb10959.x |
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| 520 | |a Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied successfully in recent GABAergic 36Cr flux measurements. NO 328, a GABA reuptake inhibitor, was included in the binding assays to prevent the uptake of [3H]muscimol. Under these conditions, the equilibrium dissociation constant (Kd) values for [3H]muscimol and [3H]-diazepam binding are 1.9 μM 40 nM, respectively. Binding affinities for these and other GABA and benzodiazepine agonists and antagonists correlate well with the known physiological doses required to elicit functional activity. This new in vitro binding protocol coupled with 36C1− flux studies should prove to be of value in reassessing the pharmacology of the GABAA receptor complex in a more physiological environment. | ||
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10.1111/j.1471-4159.1992.tb10959.x doi (DE-627)NLEJ240256573 DE-627 ger DE-627 rakwb DeLorey, Timothy M. verfasserin aut γ-Aminobutyric AcidA Receptor Pharmacology in Rat Cerebral Cortical Synaptoneurosomes Oxford, UK Blackwell Publishing Ltd 1992 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied successfully in recent GABAergic 36Cr flux measurements. NO 328, a GABA reuptake inhibitor, was included in the binding assays to prevent the uptake of [3H]muscimol. Under these conditions, the equilibrium dissociation constant (Kd) values for [3H]muscimol and [3H]-diazepam binding are 1.9 μM 40 nM, respectively. Binding affinities for these and other GABA and benzodiazepine agonists and antagonists correlate well with the known physiological doses required to elicit functional activity. This new in vitro binding protocol coupled with 36C1− flux studies should prove to be of value in reassessing the pharmacology of the GABAA receptor complex in a more physiological environment. 2006 Blackwell Publishing Journal Backfiles 1879-2005 |2006|||||||||| γ-Aminobutyric acid Brown, George B. verfasserin aut In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 58(1992), 6, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:58 year:1992 number:6 pages:0 http://dx.doi.org/10.1111/j.1471-4159.1992.tb10959.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 58 1992 6 0 |
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10.1111/j.1471-4159.1992.tb10959.x doi (DE-627)NLEJ240256573 DE-627 ger DE-627 rakwb DeLorey, Timothy M. verfasserin aut γ-Aminobutyric AcidA Receptor Pharmacology in Rat Cerebral Cortical Synaptoneurosomes Oxford, UK Blackwell Publishing Ltd 1992 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied successfully in recent GABAergic 36Cr flux measurements. NO 328, a GABA reuptake inhibitor, was included in the binding assays to prevent the uptake of [3H]muscimol. Under these conditions, the equilibrium dissociation constant (Kd) values for [3H]muscimol and [3H]-diazepam binding are 1.9 μM 40 nM, respectively. Binding affinities for these and other GABA and benzodiazepine agonists and antagonists correlate well with the known physiological doses required to elicit functional activity. This new in vitro binding protocol coupled with 36C1− flux studies should prove to be of value in reassessing the pharmacology of the GABAA receptor complex in a more physiological environment. 2006 Blackwell Publishing Journal Backfiles 1879-2005 |2006|||||||||| γ-Aminobutyric acid Brown, George B. verfasserin aut In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 58(1992), 6, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:58 year:1992 number:6 pages:0 http://dx.doi.org/10.1111/j.1471-4159.1992.tb10959.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 58 1992 6 0 |
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10.1111/j.1471-4159.1992.tb10959.x doi (DE-627)NLEJ240256573 DE-627 ger DE-627 rakwb DeLorey, Timothy M. verfasserin aut γ-Aminobutyric AcidA Receptor Pharmacology in Rat Cerebral Cortical Synaptoneurosomes Oxford, UK Blackwell Publishing Ltd 1992 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied successfully in recent GABAergic 36Cr flux measurements. NO 328, a GABA reuptake inhibitor, was included in the binding assays to prevent the uptake of [3H]muscimol. Under these conditions, the equilibrium dissociation constant (Kd) values for [3H]muscimol and [3H]-diazepam binding are 1.9 μM 40 nM, respectively. Binding affinities for these and other GABA and benzodiazepine agonists and antagonists correlate well with the known physiological doses required to elicit functional activity. This new in vitro binding protocol coupled with 36C1− flux studies should prove to be of value in reassessing the pharmacology of the GABAA receptor complex in a more physiological environment. 2006 Blackwell Publishing Journal Backfiles 1879-2005 |2006|||||||||| γ-Aminobutyric acid Brown, George B. verfasserin aut In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 58(1992), 6, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:58 year:1992 number:6 pages:0 http://dx.doi.org/10.1111/j.1471-4159.1992.tb10959.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 58 1992 6 0 |
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10.1111/j.1471-4159.1992.tb10959.x doi (DE-627)NLEJ240256573 DE-627 ger DE-627 rakwb DeLorey, Timothy M. verfasserin aut γ-Aminobutyric AcidA Receptor Pharmacology in Rat Cerebral Cortical Synaptoneurosomes Oxford, UK Blackwell Publishing Ltd 1992 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied successfully in recent GABAergic 36Cr flux measurements. NO 328, a GABA reuptake inhibitor, was included in the binding assays to prevent the uptake of [3H]muscimol. Under these conditions, the equilibrium dissociation constant (Kd) values for [3H]muscimol and [3H]-diazepam binding are 1.9 μM 40 nM, respectively. Binding affinities for these and other GABA and benzodiazepine agonists and antagonists correlate well with the known physiological doses required to elicit functional activity. This new in vitro binding protocol coupled with 36C1− flux studies should prove to be of value in reassessing the pharmacology of the GABAA receptor complex in a more physiological environment. 2006 Blackwell Publishing Journal Backfiles 1879-2005 |2006|||||||||| γ-Aminobutyric acid Brown, George B. verfasserin aut In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 58(1992), 6, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:58 year:1992 number:6 pages:0 http://dx.doi.org/10.1111/j.1471-4159.1992.tb10959.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 58 1992 6 0 |
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10.1111/j.1471-4159.1992.tb10959.x doi (DE-627)NLEJ240256573 DE-627 ger DE-627 rakwb DeLorey, Timothy M. verfasserin aut γ-Aminobutyric AcidA Receptor Pharmacology in Rat Cerebral Cortical Synaptoneurosomes Oxford, UK Blackwell Publishing Ltd 1992 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied successfully in recent GABAergic 36Cr flux measurements. NO 328, a GABA reuptake inhibitor, was included in the binding assays to prevent the uptake of [3H]muscimol. Under these conditions, the equilibrium dissociation constant (Kd) values for [3H]muscimol and [3H]-diazepam binding are 1.9 μM 40 nM, respectively. Binding affinities for these and other GABA and benzodiazepine agonists and antagonists correlate well with the known physiological doses required to elicit functional activity. This new in vitro binding protocol coupled with 36C1− flux studies should prove to be of value in reassessing the pharmacology of the GABAA receptor complex in a more physiological environment. 2006 Blackwell Publishing Journal Backfiles 1879-2005 |2006|||||||||| γ-Aminobutyric acid Brown, George B. verfasserin aut In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 58(1992), 6, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:58 year:1992 number:6 pages:0 http://dx.doi.org/10.1111/j.1471-4159.1992.tb10959.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 58 1992 6 0 |
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Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied successfully in recent GABAergic 36Cr flux measurements. NO 328, a GABA reuptake inhibitor, was included in the binding assays to prevent the uptake of [3H]muscimol. Under these conditions, the equilibrium dissociation constant (Kd) values for [3H]muscimol and [3H]-diazepam binding are 1.9 μM 40 nM, respectively. Binding affinities for these and other GABA and benzodiazepine agonists and antagonists correlate well with the known physiological doses required to elicit functional activity. This new in vitro binding protocol coupled with 36C1− flux studies should prove to be of value in reassessing the pharmacology of the GABAA receptor complex in a more physiological environment. |
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Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied successfully in recent GABAergic 36Cr flux measurements. NO 328, a GABA reuptake inhibitor, was included in the binding assays to prevent the uptake of [3H]muscimol. Under these conditions, the equilibrium dissociation constant (Kd) values for [3H]muscimol and [3H]-diazepam binding are 1.9 μM 40 nM, respectively. Binding affinities for these and other GABA and benzodiazepine agonists and antagonists correlate well with the known physiological doses required to elicit functional activity. This new in vitro binding protocol coupled with 36C1− flux studies should prove to be of value in reassessing the pharmacology of the GABAA receptor complex in a more physiological environment. |
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Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied successfully in recent GABAergic 36Cr flux measurements. NO 328, a GABA reuptake inhibitor, was included in the binding assays to prevent the uptake of [3H]muscimol. Under these conditions, the equilibrium dissociation constant (Kd) values for [3H]muscimol and [3H]-diazepam binding are 1.9 μM 40 nM, respectively. Binding affinities for these and other GABA and benzodiazepine agonists and antagonists correlate well with the known physiological doses required to elicit functional activity. This new in vitro binding protocol coupled with 36C1− flux studies should prove to be of value in reassessing the pharmacology of the GABAA receptor complex in a more physiological environment. |
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<?xml version="1.0" encoding="UTF-8"?><collection xmlns="http://www.loc.gov/MARC21/slim"><record><leader>01000caa a22002652 4500</leader><controlfield tag="001">NLEJ240256573</controlfield><controlfield tag="003">DE-627</controlfield><controlfield tag="005">20230505204641.0</controlfield><controlfield tag="007">cr uuu---uuuuu</controlfield><controlfield tag="008">120426s1992 xx |||||o 00| ||und c</controlfield><datafield tag="024" ind1="7" ind2=" "><subfield code="a">10.1111/j.1471-4159.1992.tb10959.x</subfield><subfield code="2">doi</subfield></datafield><datafield tag="035" ind1=" " ind2=" "><subfield code="a">(DE-627)NLEJ240256573</subfield></datafield><datafield tag="040" ind1=" " ind2=" "><subfield code="a">DE-627</subfield><subfield code="b">ger</subfield><subfield code="c">DE-627</subfield><subfield code="e">rakwb</subfield></datafield><datafield tag="100" ind1="1" ind2=" "><subfield code="a">DeLorey, Timothy M.</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="245" ind1="1" ind2="0"><subfield code="a">γ-Aminobutyric AcidA Receptor Pharmacology in Rat Cerebral Cortical Synaptoneurosomes</subfield></datafield><datafield tag="264" ind1=" " ind2="1"><subfield code="a">Oxford, UK</subfield><subfield code="b">Blackwell Publishing Ltd</subfield><subfield code="c">1992</subfield></datafield><datafield tag="300" ind1=" " ind2=" "><subfield code="a">Online-Ressource</subfield></datafield><datafield tag="336" ind1=" " ind2=" "><subfield code="a">nicht spezifiziert</subfield><subfield code="b">zzz</subfield><subfield code="2">rdacontent</subfield></datafield><datafield tag="337" ind1=" " ind2=" "><subfield code="a">nicht spezifiziert</subfield><subfield code="b">z</subfield><subfield code="2">rdamedia</subfield></datafield><datafield tag="338" ind1=" " ind2=" "><subfield code="a">nicht spezifiziert</subfield><subfield code="b">zu</subfield><subfield code="2">rdacarrier</subfield></datafield><datafield tag="520" ind1=" " ind2=" "><subfield code="a">Abstract: Equilibrium binding interactions at the γ-amino-butyric acid (GABA) and benzodiazepine recognition sites on the GABAA receptor-Cl− ionophore complex were studied using a vesicular synaptoneurosome (microsacs) preparation of rat brain in a physiological HEPES buffer similar to that applied successfully in recent GABAergic 36Cr flux measurements. NO 328, a GABA reuptake inhibitor, was included in the binding assays to prevent the uptake of [3H]muscimol. Under these conditions, the equilibrium dissociation constant (Kd) values for [3H]muscimol and [3H]-diazepam binding are 1.9 μM 40 nM, respectively. Binding affinities for these and other GABA and benzodiazepine agonists and antagonists correlate well with the known physiological doses required to elicit functional activity. This new in vitro binding protocol coupled with 36C1− flux studies should prove to be of value in reassessing the pharmacology of the GABAA receptor complex in a more physiological environment.</subfield></datafield><datafield tag="533" ind1=" " ind2=" "><subfield code="d">2006</subfield><subfield code="f">Blackwell Publishing Journal Backfiles 1879-2005</subfield><subfield code="7">|2006||||||||||</subfield></datafield><datafield tag="650" ind1=" " ind2="4"><subfield code="a">γ-Aminobutyric acid</subfield></datafield><datafield tag="700" ind1="1" ind2=" "><subfield code="a">Brown, George B.</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="773" ind1="0" ind2="8"><subfield code="i">In</subfield><subfield code="t">Journal of neurochemistry</subfield><subfield code="d">Oxford : Wiley-Blackwell, 1956</subfield><subfield code="g">58(1992), 6, Seite 0</subfield><subfield code="h">Online-Ressource</subfield><subfield code="w">(DE-627)NLEJ243927584</subfield><subfield code="w">(DE-600)2020528-4</subfield><subfield code="x">1471-4159</subfield><subfield code="7">nnns</subfield></datafield><datafield tag="773" ind1="1" ind2="8"><subfield code="g">volume:58</subfield><subfield code="g">year:1992</subfield><subfield code="g">number:6</subfield><subfield code="g">pages:0</subfield></datafield><datafield tag="856" ind1="4" ind2="0"><subfield code="u">http://dx.doi.org/10.1111/j.1471-4159.1992.tb10959.x</subfield><subfield code="q">text/html</subfield><subfield code="x">Verlag</subfield><subfield code="z">Deutschlandweit zugänglich</subfield><subfield code="3">Volltext</subfield></datafield><datafield tag="912" ind1=" " ind2=" "><subfield code="a">GBV_USEFLAG_U</subfield></datafield><datafield tag="912" ind1=" " ind2=" "><subfield code="a">ZDB-1-DJB</subfield></datafield><datafield tag="912" ind1=" " ind2=" "><subfield code="a">GBV_NL_ARTICLE</subfield></datafield><datafield tag="951" ind1=" " ind2=" "><subfield code="a">AR</subfield></datafield><datafield tag="952" ind1=" " ind2=" "><subfield code="d">58</subfield><subfield code="j">1992</subfield><subfield code="e">6</subfield><subfield code="h">0</subfield></datafield></record></collection>
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7.401639 |