胆囊收缩素（CCK）受体拮抗剂MK-329和L-365,260对大鼠迷走神经上轴突运输的CCK结合位点的选择性。
Selectivity of cholecystokinin (CCK) receptor antagonists, MK-329 and L-365,260, for axonally-transported CCK binding sites on the rat vagus nerve.
作者信息
Mercer J G, Lawrence C B
机构信息
Rowett Research Institute, Bucksburn, Aberdeen, UK.
出版信息
Neurosci Lett. 1992 Mar 30;137(2):229-31. doi: 10.1016/0304-3940(92)90410-9.
The ability of the cholecystokinin (CCK) receptor antagonists, MK-329 and L-365,260, to selectively inhibit 125I-Bolton-Hunter-CCK8 binding to ligated rat vagus nerve in vitro was examined at concentrations ranging from 10(-10) M to 10(-6) M. Both antagonists inhibited binding to CCK binding sites accumulating proximal to ligatures on the cervical vagus. Incubation of nerve sections in the presence of both antagonists produced an additive effect, indicating that both CCK-A and CCK-B binding sites are transported towards the periphery. In contrast, CCK binding sites accumulating distal to the ligature possessed the pharmacological characteristics of the CCK-B receptor sub-type only.
在10⁻¹⁰ M至10⁻⁶ M的浓度范围内，研究了胆囊收缩素（CCK）受体拮抗剂MK - 329和L - 365,260在体外选择性抑制¹²⁵I - 博尔顿 - 亨特 - CCK8与结扎大鼠迷走神经结合的能力。两种拮抗剂均抑制与颈迷走神经结扎近端积累的CCK结合位点的结合。在两种拮抗剂存在下孵育神经切片产生了相加效应，表明CCK - A和CCK - B结合位点都向周围运输。相反，结扎远端积累的CCK结合位点仅具有CCK - B受体亚型的药理学特征。
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