Knight A R, Wyatt C, Middlemiss D N
Merck Sharp and Dohme, Neuroscience Research Centre, Harlow, Essex.
Neuropharmacology. 1991 Aug;30(8):923-5. doi: 10.1016/0028-3908(91)90128-x.
The effect of dosing guinea pigs with spironolactone (100 mg/kg twice daily for 3 days) upon the sigma recognition site labelled with [3H]-DTG was investigated. Animals were dosed with 100 mg/kg spironolactone twice a day for 3 days. Spironolactone treatment caused a decrease in sigma radioligand binding in membranes prepared from liver and brain but not in adrenals or testes. Saturation analysis of [3H]-DTG radioligand binding in the brain indicated that the decrease in specifically bound [3H]-DTG binding was due to a reduction in receptor number with no change in affinity. This method for the selective depletion of brain and liver sigma recognition sites will provide a useful tool for exploring the functional significance of this site.
研究了给豚鼠服用螺内酯（100毫克/千克，每日两次，共3天）对用[3H]-DTG标记的西格玛识别位点的影响。动物每日两次服用100毫克/千克螺内酯，共3天。螺内酯处理导致从肝脏和大脑制备的膜中西格玛放射性配体结合减少，但肾上腺或睾丸中未减少。对大脑中[3H]-DTG放射性配体结合的饱和分析表明，特异性结合的[3H]-DTG结合减少是由于受体数量减少，亲和力无变化。这种选择性消耗大脑和肝脏西格玛识别位点的方法将为探索该位点的功能意义提供一个有用的工具。
