Bennett Marco A, Murray Thomas F, Aldrich Jane V
Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, Maryland 21201, USA.
J Med Chem. 2002 Dec 19;45(26):5617-9. doi: 10.1021/jm025575g.
Arodyn (aromatic dynorphin) is a novel analogue of the opioid peptide dynorphin A with a nonbasic N-terminus that exhibits nanomolar affinity (K(i) = 10 nM) and remarkable selectivity for kappa opioid receptors (K(i) ratio (kappa/mu/delta) = 1/174/583). Arodyn completely reverses the agonism of dynorphin A (1-13)NH(2) in a concentration-dependent manner in the adenylyl cyclase assay. Thus arodyn is a novel kappa opioid receptor selective antagonist that will be useful to study these receptors.
阿罗丁（芳香强啡肽）是阿片肽强啡肽A的一种新型类似物，其N端无碱性基团，对κ阿片受体表现出纳摩尔亲和力（K(i)=10 nM）和显著选择性（K(i)比值（κ/μ/δ）=1/174/583）。在腺苷酸环化酶测定中，阿罗丁以浓度依赖的方式完全逆转强啡肽A（1-13）NH(2)的激动作用。因此，阿罗丁是一种新型的κ阿片受体选择性拮抗剂，将有助于研究这些受体。
