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Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABA receptors.

Biochem. Pharmacol.. 2018-08; 
SöderhielmPella Cecilia,BalleThomas,Bak-NyhusSøren,ZhangMichael,HansenKaroline M,AhringPhilip K,JensenAnde
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ORF cDNA Clones/MolecularCloud … The cDNA encoding for the trimeric concatenated subunit constructs β 2 -α 1 -β 2 and β 2 -α 3 -β 2 (both subcloned into the pCDNA3.1 vector using the restriction enzymes XhoI and XbaI) were purchased from GenScript (Piscataway, NJ) … Get A Quote

摘要

The extracellular α/γ interface in the αβγ GABA receptor harbours the allosteric binding site targeted by benzodiazepines and newer generations of subtype-selective modulators. We have probed the molecular determinants for the affinity/potency-based α-preference exhibited by the hypnotic zolpidem (Ambien®, Stilnox®) and the efficacy-based α-over-α selectivity displayed by the analgesic NS11394. Binding affinities and functional properties of the modulators were characterized at wild-type, concatenated, mutant and chimeric αβγ receptors expressed in tsA201 cells and Xenopus oocytes by [H]flumazenil binding and two-electrode voltage clamp electrophysiology. Substitution of Gly in α with the co... More

关键词

Allosteric modulation,Benzodiazepine site,GABA(A) receptors,Indiplon,L-838,417,NS11394,Positive allosteric modulator,Subtype-selectivity,Zolp