CiNii 博士論文 - RGS4 regulates partial agonism of the M2 muscarinic receptor-activated K⁺
currents … RGS4 regulates partial agonism of the M2 muscarinic receptor-activated K⁺
currents RSG4タンパク質はムスカリンM2受容体活性化カリウム電流におけるパーシャル
アゴニスト作用を制御する … RGS4 regulates partial agonism of the M2 muscarinic receptor-activated
K⁺ currents …

Key points Partial agonists produce a smaller response than full agonists even at 100%
receptor occupancy. In G‐protein‐coupled receptor signalling, the submaximal efficacy of
partial agonists is determined by the conformational change of the agonist–receptor
complex, which reduces effector activation. However, it remains unclear whether the
regulator of G‐protein signalling (RGS) proteins contribute to the partial agonism. By
analysing the M2 muscarinic receptor (M2R)‐activated G‐protein‐gated K+ inwardly …