BAM 18的药理学特征。
The pharmacological profile of BAM 18.
作者信息
Hurlbut D E, Evans C J, Barchas J D, Leslie F M
机构信息
Department of Pharmacology, University of California, Irvine 92715.
出版信息
NIDA Res Monogr. 1986;75:81-4.
The opioid receptor selectivity of BAM 18 was determined by radioligand binding and peripheral tissue bioassay. Using selective radioligand binding conditions, BAM 18 bound to the mu opioid receptor with an affinity twice that of the K receptor and over 10 times that of the delta opioid receptor (Ki = 0.29, 0.84 and 3.9 nM, respectively). Ke values for naloxone antagonism of BAM 18 activity in the electrically stimulated guinea pig ileum and the mouse vas deferens were 4.3 and 9.9 nM respectively. The pharmacological profile of BAM 18 was similar to that of metorphamide.
通过放射性配体结合和外周组织生物测定法确定了BAM 18的阿片受体选择性。在选择性放射性配体结合条件下，BAM 18与μ阿片受体结合，其亲和力是κ受体的两倍，是δ阿片受体的10倍以上（Ki分别为0.29、0.84和3.9 nM）。在电刺激的豚鼠回肠和小鼠输精管中，纳洛酮拮抗BAM 18活性的Ke值分别为4.3和9.9 nM。BAM 18的药理学特征与美托啡肽相似。
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