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

39 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

Access to Document

10.1021/jm025575g

Cite this

@article{adf55275f1394d5b8ec6260c17895a7c,

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

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.",

author = "Bennett, {Marco A.} and Murray, {Thomas F.} and Aldrich, {Jane V.}",

year = "2002",

month = dec,

day = "19",

doi = "10.1021/jm025575g",

language = "English (US)",

volume = "45",

pages = "5617--5619",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "26",

}

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.

UR - http://www.scopus.com/inward/record.url?scp=0037137590&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0037137590&partnerID=8YFLogxK

U2 - 10.1021/jm025575g

DO - 10.1021/jm025575g

M3 - Article

C2 - 12477343

AN - SCOPUS:0037137590

VL - 45

SP - 5617

EP - 5619

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 26

ER -

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

Abstract

All Science Journal Classification (ASJC) codes

Access to Document

Other files and links

Fingerprint

Cite this