Delay-Goyet P, Zajac J M, Roques B P
U266 INSERM, UA 498 CNRS, Département de Chimie Organique, Faculté de Pharmacie, Paris, France.
Neurosci Lett. 1989 Aug 28;103(2):197-202. doi: 10.1016/0304-3940(89)90575-2.
Neutral endopeptidase (NEP) and mu- and delta-opioid receptor densities were measured in sections of rat striatum by in vitro radioautography with the selective ligands: 3 nM [3H]N-[(2RS)-3-hydroxyaminocarbonyl-2-benzyl-1-oxopropyl]glycine ([ 3H]HACBO-Gly), 3 nM [3H]Tyr-D.Ala-Gly-(NMe)Phe-Gly-ol ([ 3H]DAGO) and 3 nM [3H]Tyr-D-Thr-Gly-Phe-Leu-Thr ([ 3H]DTLET), respectively. Haloperidol treatment (2 mg/kg/day, i.p., 3 weeks), which has been reported to increase enkephalin levels in the striatum, induced a 23% decrease in striatal (posterior level A= +8.4-8.6 mm) NEP labeling (but no change of mu- and delta-sites). In contrast, no change in NEP occurred after chronic morphine (40-160 mg/kg/day, s.c., 4 days) or kelatorphan (10 nmol/h, i.c.v., 7 days), a mixed inhibitor of enkephalin-degrading peptidases.
通过体外放射自显影法，使用选择性配体分别为3 nM [3H]N-[(2RS)-3-羟基氨基羰基-2-苄基-1-氧代丙基]甘氨酸（[3H]HACBO-Gly）、3 nM [3H]酪氨酰-D-丙氨酰-甘氨酰-（N-甲基）苯丙氨酰-甘氨醇（[3H]DAGO）和3 nM [3H]酪氨酰-D-苏氨酰-甘氨酰-苯丙氨酰-亮氨酰-苏氨酸（[3H]DTLET），测量大鼠纹状体切片中的中性内肽酶（NEP）以及μ和δ阿片受体密度。据报道，氟哌啶醇治疗（2 mg/kg/天，腹腔注射，3周）可增加纹状体中脑啡肽水平，该治疗导致纹状体（后水平A = +8.4 - 8.6 mm）NEP标记减少23%（但μ和δ位点无变化）。相比之下，慢性吗啡（40 - 160 mg/kg/天，皮下注射，4天）或凯拉托芬（10 nmol/h，脑室内注射，7天，脑啡肽降解肽的混合抑制剂）治疗后，NEP无变化。
