A highly selective κ-opioid receptor agonist with low addictive potential and dependence liability

Hee Sock Park; Hee Yoon Lee; Yong Hae Kim; Jin Kyu Park; Edwin E. Zvartau; Heeseung Lee

doi:10.1016/j.bmcl.2006.02.017

A highly selective κ-opioid receptor agonist with low addictive potential and dependence liability

Hee Sock Park, Hee Yoon Lee, Yong Hae Kim, Jin Kyu Park, Edwin E. Zvartau, Heeseung Lee

Department of Anesthesia and Pain Medicine

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

13 Scopus citations

Abstract

Buprenorphine analogs have been synthesized. In the studies of analgesic and addictive effects in mice and [³⁵S]GTPγS binding assay in human brain tissue, an analog of buprenorphine where the tert-butyl is replaced by a cyclobutyl moiety (16) has been identified as a selective κ-partial agonist which gives antinociceptive effects, but has low abuse potential. The results may lead to lower degrees of dysphoria than full κ-agonists.

Original language	English
Pages (from-to)	3609-3613
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	13
DOIs	https://doi.org/10.1016/j.bmcl.2006.02.017
State	Published - 1 Jul 2006

Keywords

κ-partial agonist
Addiction
Buprenorphine
Opioid

Access to Document

10.1016/j.bmcl.2006.02.017

Cite this

@article{2ee8aa11bae74d3685c46747d39b6a6c,

title = "A highly selective κ-opioid receptor agonist with low addictive potential and dependence liability",

abstract = "Buprenorphine analogs have been synthesized. In the studies of analgesic and addictive effects in mice and [35S]GTPγS binding assay in human brain tissue, an analog of buprenorphine where the tert-butyl is replaced by a cyclobutyl moiety (16) has been identified as a selective κ-partial agonist which gives antinociceptive effects, but has low abuse potential. The results may lead to lower degrees of dysphoria than full κ-agonists.",

keywords = "κ-partial agonist, Addiction, Buprenorphine, Opioid",

author = "Park, {Hee Sock} and Lee, {Hee Yoon} and Kim, {Yong Hae} and Park, {Jin Kyu} and Zvartau, {Edwin E.} and Heeseung Lee",

year = "2006",

month = jul,

day = "1",

doi = "10.1016/j.bmcl.2006.02.017",

language = "English",

volume = "16",

pages = "3609--3613",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

number = "13",

}

TY - JOUR

T1 - A highly selective κ-opioid receptor agonist with low addictive potential and dependence liability

AU - Park, Hee Sock

AU - Lee, Hee Yoon

AU - Kim, Yong Hae

AU - Park, Jin Kyu

AU - Zvartau, Edwin E.

AU - Lee, Heeseung

PY - 2006/7/1

Y1 - 2006/7/1

N2 - Buprenorphine analogs have been synthesized. In the studies of analgesic and addictive effects in mice and [35S]GTPγS binding assay in human brain tissue, an analog of buprenorphine where the tert-butyl is replaced by a cyclobutyl moiety (16) has been identified as a selective κ-partial agonist which gives antinociceptive effects, but has low abuse potential. The results may lead to lower degrees of dysphoria than full κ-agonists.

AB - Buprenorphine analogs have been synthesized. In the studies of analgesic and addictive effects in mice and [35S]GTPγS binding assay in human brain tissue, an analog of buprenorphine where the tert-butyl is replaced by a cyclobutyl moiety (16) has been identified as a selective κ-partial agonist which gives antinociceptive effects, but has low abuse potential. The results may lead to lower degrees of dysphoria than full κ-agonists.

KW - κ-partial agonist

KW - Addiction

KW - Buprenorphine

KW - Opioid

UR - http://www.scopus.com/inward/record.url?scp=33646833956&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2006.02.017

DO - 10.1016/j.bmcl.2006.02.017

M3 - Article

C2 - 16650985

AN - SCOPUS:33646833956

VL - 16

SP - 3609

EP - 3613

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 13

ER -

A highly selective κ-opioid receptor agonist with low addictive potential and dependence liability

Abstract

Keywords

Access to Document

Fingerprint

Cite this