Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 26, Pages 5617-5619Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm025575g
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Funding
- NIDA NIH HHS [R01 DA05195, F01 DA15029] Funding Source: Medline
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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)NH2 in a concentration-dependent manner in the adenylyl cyclase assay. Thus arodyn is a novel K opioid receptor selective antagonist that will be useful to study these receptors.
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