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510365 [2018/11/20 14:26] (current)
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 +====== The gamma-aminobutyrate/​benzodiazepine receptor from pig brain. Enhancement of gamma-aminobutyrate-receptor binding by the anaesthetic propanidid.======
 +
 +** Article date:** 1986/1/1
 +~~META:date created = 1986-01-01~~
 +
 +** PubMed ID: 510365 **
 +
 +** Journal name: The Biochemical journal (ISSN: 0264-6021) **
 +
 +** ABSTRACT **
 +
 +The binding of [3H]muscimol,​ a gamma-aminobutyrate (GABA) receptor agonist, to a membrane preparation from pig cerebral cortex was enhanced by the anaesthetic propanidid in a concentration-dependent manner. At 0 degrees C, binding was stimulated to 220% of control values, with 50% stimulation at 60 microM-propanidid. At 37 degrees C, propanidid caused a more powerful stimulation of [3H]muscimol binding (340% of control values). Propanidid (1 mM) exerted little effect on the affinity of muscimol binding (KD approx. 10 nM), but increased the apparent number of high-affinity binding sites in the membrane by 2-fold. Enhancement of [3H]muscimol binding was observed only in the presence of Cl- ions, half-maximal activation being achieved at approx. 40 mM-Cl-. Picrotoxinin inhibited the stimulation of [3H]muscimol binding by propanidid with an IC50 (concentration causing 50% inhibition) value of approx. 25 microM. The enhancement of [3H]muscimol binding by propanidid was not additive with the enhancement produced by secobarbital. Phenobarbital inhibited the effect of propanidid and secobarbital. The GABA receptor was solubilized with Triton X-100 or with Chaps [3-[(3-cholamidopropyl)dimethylammonio]propanesulphonate]. Propanidid and secobarbital did not stimulate the binding of [3H]muscimol after solubilization with Triton X-100. However, the receptor could be solubilized by 5 mM-Chaps with retention of the stimulatory effects of propanidid and secobarbital. Unlike barbiturates,​ propanidid did not stimulate the binding of [3H]flunitrazepam to membranes. It is suggested that the ability to modulate the [3H]muscimol site of the GABA-receptor complex may be a common and perhaps functional characteristic of general anaesthetics.
 +
 +===== ===== 
 +
 +Author List: Kirkness E F, Turner A J
 +
 +Publication Types: Journal Article; Research Support, Non-U.S. Gov't
 +
 +Substances mentioned in the article: Receptors, GABA-A; Picrotoxin; Secobarbital;​ Muscimol; Potassium Chloride; Propanidid; ​
 +
 +Mesh terms: Animals; Brain/​metabolism;​ Kinetics; Muscimol/​metabolism;​ Picrotoxin/​pharmacology;​ Potassium Chloride/​pharmacology;​ Propanidid/​pharmacology;​ Receptors, GABA-A/drug effects; Secobarbital/​pharmacology;​ Swine; Synaptic Membranes/​metabolism; ​
 +
 +Citations: ​  - //​[[491857]]//​
 +  - //​[[223555]]//​
 +  - //​[[6103810]]//​
 +  - //​[[6261261]]//​
 +  - //​[[6265597]]//​
 +  - //​[[6269691]]//​
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 +  - //​[[6271925]]//​
 +  - //​[[6273918]]//​
 +  - //​[[7321780]]//​
 +  - //​[[6277679]]//​
 +  - //​[[7050308]]//​
 +  - //​[[6291550]]//​
 +  - //​[[6292364]]//​
 +  - //​[[6292381]]//​
 +  - //​[[6133516]]//​
 +  - //​[[6308160]]//​
 +  - //​[[6308164]]//​
 +  - //​[[6308170]]//​
 +  - //​[[6314189]]//​
 +  - //​[[6318143]]//​
 +  - //​[[2981283]]//​
 +  - //​[[6098342]]//​
 +  - //​[[6099281]]//​
 +  - //​[[3006661]]//​
 +  - //​[[14907713]]//​
 +  - //​[[4871804]]//​
 +  - //​[[4913408]]//​
 +  - //​[[876033]]//​
 +  - //​[[207386]]//​
 +  - //​[[738408]]//​
 +  - //​[[378102]]//​
 +  - //​[[510365]]//​
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 +{{tag> Potassium_Chloride Receptors,​_GABA-A Secobarbital Picrotoxin Propanidid Muscimol }}
 +
 +{{keywords>​ Potassium Chloride, Receptors, GABA-A, Secobarbital,​ Picrotoxin, Propanidid, Muscimol}}
 +
  
510365.txt ยท Last modified: 2018/11/20 14:26 (external edit)