5-甲基糠甲醚在毒蕈碱受体上的表观活性。
Apparent activity of 5-methylfurmethide at muscarinic receptors.
作者信息
Ochillo R F
出版信息
Arch Int Pharmacodyn Ther. 1980 Nov;248(1):69-75.
Apparent activity of 5-methylfurfuryltrimethylammonium iodide (5-methylfurmethide, 5-MFT) at muscarinic receptors of the ileal longitudinal muscle of the guinea-pig was investigated. These parameters were determined by the analysis of concentration-response data before and after fractional inactivation of receptors by phenoxybenzamine, an irreversible receptor blocker. The apparent ED50, dissociation constant (KA), and relative affinity (in comparison to acetylcholine, ACh) were 2.75 +/- 0.22 X 10(-8) M, 7.22 +/- 0.15 X 10(-7) M and 1.33 respectively. The relative intrinsic efficacy compared to ACh was 1.54.
研究了5-甲基糠基三甲基碘化铵（5-甲基糠铵，5-MFT）对豚鼠回肠纵肌毒蕈碱受体的表观活性。通过分析在用不可逆受体阻滞剂苯氧苄胺使受体部分失活前后的浓度-反应数据来确定这些参数。表观半数有效浓度（ED50）、解离常数（KA）和相对亲和力（与乙酰胆碱，ACh相比）分别为2.75±0.22×10⁻⁸ M、7.22±0.15×10⁻⁷ M和1.33。与ACh相比，相对内在活性为1.54。
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