Identification of arodyn, a novel acetylated dynorphin a-(1-11) analogue, as a κ opioid receptor antagonist

Marco A. Bennett; Thomas F. Murray; Jane V. Aldrich

doi:10.1021/jm025575g

Identification of arodyn, a novel acetylated dynorphin a-(1-11) analogue, as a κ opioid receptor antagonist

Marco A. Bennett, Thomas F. Murray, Jane V. Aldrich

Research output: Contribution to journal › Article › peer-review

40 Scopus citations

Abstract

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 κ opioid receptors (K_i 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	https://doi.org/10.1021/jm025575g
State	Published - Dec 19 2002
Externally published	Yes

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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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.",

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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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Identification of arodyn, a novel acetylated dynorphin a-(1-11) analogue, as a κ opioid receptor antagonist

Abstract

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