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 |
|---|---|
| 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 |
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All Science Journal Classification (ASJC) codes
- Organic Chemistry
Cite this
Identification of arodyn, a novel acetylated dynorphin a-(1-11) analogue, as a κ opioid receptor antagonist. / Bennett, Marco A.; Murray, Thomas F.; Aldrich, Jane V.
In: Journal of Medicinal Chemistry, Vol. 45, No. 26, 19.12.2002, p. 5617-5619.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Identification of arodyn, a novel acetylated dynorphin a-(1-11) analogue, as a κ opioid receptor antagonist
AU - Bennett, Marco A.
AU - Murray, Thomas F.
AU - Aldrich, Jane V.
PY - 2002/12/19
Y1 - 2002/12/19
N2 - 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.
AB - 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.
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UR - http://www.scopus.com/inward/citedby.url?scp=0037137590&partnerID=8YFLogxK
U2 - 10.1021/jm025575g
DO - 10.1021/jm025575g
M3 - Article
VL - 45
SP - 5617
EP - 5619
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 26
ER -