Nielsen M, Witt M R, Ebert B, Krogsgaard-Larsen P
Department of Biochemistry, St. Hans Hospital, Roskilde, Denmark.
Eur J Pharmacol. 1995 Mar 15;289(1):109-12. doi: 10.1016/0922-4106(95)90175-2.
Thiomuscimol inhibits [3H]muscimol binding to brain GABAA receptors. Exposure of Ag(+)-treated membrane preparations to UV radiation at 254 nm for 40 min in the presence of thiomuscimol (10(-5) M) produced a 20-30% irreversible decrease in high-affinity [3H]muscimol binding sites. The photoaffinity labeling of thiomuscimol was inhibited by GABA (10(-4) M) added prior to exposure to UV light. The data show that thiomuscimol can label the GABAA receptor site and that the ligand can be used as a photoaffinity label for purification and identification of GABA binding sites within the GABAA receptor complex.
硫代蝇蕈醇抑制[³H]蝇蕈醇与脑GABAA受体的结合。在硫代蝇蕈醇（10⁻⁵ M）存在的情况下，将经Ag(+)处理的膜制剂在254 nm紫外线下照射40分钟，导致高亲和力[³H]蝇蕈醇结合位点不可逆地减少20 - 30%。在暴露于紫外线之前加入的GABA（10⁻⁴ M）可抑制硫代蝇蕈醇的光亲和标记。数据表明，硫代蝇蕈醇可标记GABAA受体位点，且该配体可作为光亲和标记物用于纯化和鉴定GABAA受体复合物中的GABA结合位点。
