Abstract
Arodyn (aromatic dynorphin) is a novel analogue of the opioid peptide dynorphin A with a nonbasic N-terminus that exhibits nanomolar affinity (Ki = 10 nM) and remarkable selectivity for κ opioid receptors (Ki ratio (κ/μ/δ) = 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 κ opioid receptor selective antagonist that will be useful to study these receptors.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 5617-5619 |
| Number of pages | 3 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 45 |
| Issue number | 26 |
| DOIs | |
| State | Published - Dec 19 2002 |
| Externally published | Yes |
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Drug Discovery
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Bennett, M. A., Murray, T. F., & Aldrich, J. V. (2002). Identification of arodyn, a novel acetylated dynorphin a-(1-11) analogue, as a κ opioid receptor antagonist. Journal of Medicinal Chemistry, 45(26), 5617-5619. https://doi.org/10.1021/jm025575g