Waksman G, Bouboutou R, Devin J, Besselievre R, Fournie-Zaluski M C, Roques B P
Biochem Biophys Res Commun. 1985 Aug 30;131(1):262-8. doi: 10.1016/0006-291x(85)91797-8.
The synthesis and binding properties to rat brain tissue of the enkephalinase inhibitor [3H] N-[(R,S)-3-hydroxyaminocarbonyl-2-benzyl-1-oxopropyl]-glycine ([3H]HACBO-Gly, 45 Ci/mmole) is reported. [3H]HACBO-Gly binding to membranes from various rat brain tissue is saturable (KD = 0.4 +/- 0.05 nM) and linearly related to the amount of tissue. Non specific binding is less than 15% of total binding at the KD concentration. The regional distribution of [3H]HACBO-Gly binding and enkephalinase activity are closely correlated with highest levels in striatum and substantia nigra. The efficiency of inhibitors of various peptidases (thiorphan, captopril, bestatin ...) to inhibit [3H]HACBO-Gly binding or enkephalinase activity are similar. These results indicate that [3H]HACBO-Gly binds selectively to enkephalinase. This compound should help to clarify the localization of the enzyme in the CNS.
本文报道了脑啡肽酶抑制剂[3H]N-[(R,S)-3-羟基氨基羰基-2-苄基-1-氧代丙基]-甘氨酸([3H]HACBO-Gly，45居里/毫摩尔)的合成及其与大鼠脑组织的结合特性。[3H]HACBO-Gly与大鼠不同脑组织的膜结合具有饱和性(KD = 0.4±0.05纳摩尔)，且与组织量呈线性关系。在KD浓度下，非特异性结合小于总结合的15%。[3H]HACBO-Gly结合的区域分布和脑啡肽酶活性密切相关，纹状体和黑质中的水平最高。各种肽酶抑制剂(硫磷酰胺、卡托普利、贝司他汀……)抑制[3H]HACBO-Gly结合或脑啡肽酶活性的效率相似。这些结果表明[3H]HACBO-Gly选择性地与脑啡肽酶结合。该化合物应有助于阐明该酶在中枢神经系统中的定位。
