Zhang K, Tarazi F I, Kula N S, Baldessarini R J, Neumeyer J L
Neuropharmacology Laboratory, Mailman Research Center, McLean Division of Massachusetts General Hospital, Belmont 02478, USA.
Neurosci Lett. 1999 Oct 29;274(3):155-8. doi: 10.1016/s0304-3940(99)00700-4.
Effects of the D2-like receptor alkylating agent NIPS (N-[p-isothiocyanatophenethyl]spiperone) on dopamine receptors in rat brain were characterized by radioreceptor assays and quantitative autoradiography. NIPS alkylated D2 and D4 receptors concentration-dependently in brain sections and transfected cells. NIPS also alkylated both receptors dose-dependently in vivo, with no effect on dopamine D1-like or serotonin 5-HT2 receptors at a dose that occluded 75% of D2 and D4 receptors. Pretreatment with D2-like receptor selective antagonist haloperidol completely blocked the effects of NIPS. The findings demonstrate that NIPS selectively alkylates D2 and D4 receptors, indicating its potential utility for studies of these receptors.
通过放射受体分析和定量放射自显影法对D2样受体烷基化剂NIPS（N-[对异硫氰酸苯乙基]螺哌隆）对大鼠脑内多巴胺受体的作用进行了表征。NIPS在脑切片和转染细胞中浓度依赖性地烷基化D2和D4受体。NIPS在体内也剂量依赖性地烷基化这两种受体，在阻断75%的D2和D4受体的剂量下，对多巴胺D1样受体或5-羟色胺5-HT2受体没有影响。用D2样受体选择性拮抗剂氟哌啶醇预处理可完全阻断NIPS的作用。这些发现表明NIPS选择性地烷基化D2和D4受体，表明其在这些受体研究中的潜在用途。
