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 journalArticle

35 Citations (Scopus)

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 languageEnglish
Pages (from-to)5617-5619
Number of pages3
JournalJournal of Medicinal Chemistry
Volume45
Issue number26
DOIs
StatePublished - Dec 19 2002
Externally publishedYes

Fingerprint

Dynorphins
Narcotic Antagonists
Opioid Receptors
Opioid Peptides
Adenylyl Cyclases
Assays
arodyn
dynorphin (1-11)

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 journalArticle

@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 = "12",
day = "19",
doi = "10.1021/jm025575g",
language = "English",
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

VL - 45

SP - 5617

EP - 5619

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 26

ER -