Shi, An-Guo’s team published research in Journal of Pharmacology and Experimental Therapeutics in 271 | CAS: 70539-42-3

Journal of Pharmacology and Experimental Therapeutics published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C25H47NO8, Synthetic Route of 70539-42-3.

Shi, An-Guo published the artcilePrecoupling of alpha-2B adrenergic receptors and G-proteins in transfected PC-12 cell membranes: influence of pertussis toxin and a lysine-directed cross-linker, Synthetic Route of 70539-42-3, the publication is Journal of Pharmacology and Experimental Therapeutics (1994), 271(3), 1520-7, database is CAplus and MEDLINE.

The ability of pertussis toxin (PTX) pretreatment to alter the binding of [3H]rauwolscine (RAU) to alpha-2B adrenergic receptors expressed in PC12 cells was examined PTX caused a 30% increase in the Bmax for [3H]RAU and reduced its KD, whereas in the added presence of Na+ and Gpp(NH)p binding was increased to 75% above the level in untreated membranes. Because all three agents act to reduce receptor/G-protein affinity, the increased binding may reflect extensive precoupling of the alpha-2B receptor. The affinity of the agonist epinephrine in displacing [3H]RAU was normally reduced by both Na+ and Gpp(NH)p; however, in PTX-treated membranes the effect of Gpp(NH)p was eliminated, and Na+ remained effective. The lysine-directed crosslinking reagent ethyleneglycol bis(succinimidyl)succinate (EGS) was utilized to cross-link precoupled receptor and G-protein. Maximal [3H]RAU binding was reduced by EGS in a time- and dose-dependent manner, and this action was reversed by prior incubation with Na+ and Gpp(NH)p, suggesting that EGS did indeed cross-link receptor and G-protein. RAU and epinephrine each provided protection against the effect of EGS. The inclusion of Na+ and Gpp(NH)p during [3H]RAU binding studies was able to restore maximal binding in EGS-treated membranes to the same level as untreated membranes. These results indicate that in the absence of Na+ and Gpp(NH)p at least 40% of the total alpha-2B adrenergic receptors in these membranes exist as a precoupled receptor/G-protein complex which fails to bind [3H]RAU.

Journal of Pharmacology and Experimental Therapeutics published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C25H47NO8, Synthetic Route of 70539-42-3.

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