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

15 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

Addiction
Buprenorphine
Opioid
κ-partial agonist

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10.1016/j.bmcl.2006.02.017

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

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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 - Addiction

KW - Buprenorphine

KW - Opioid

KW - κ-partial agonist

UR - https://www.scopus.com/pages/publications/33646833956

U2 - 10.1016/j.bmcl.2006.02.017

DO - 10.1016/j.bmcl.2006.02.017

M3 - Article

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AN - SCOPUS:33646833956

SN - 0960-894X

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SP - 3609

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 13

ER -

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

Abstract

Keywords

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