Selective δ-opioid receptor ligands: potential PET ligands based on naltrindole

J Clayson; A R Jales; R J Tyacke; A L Hudson; D J Nutt; J W Lewis; S M Husbands

doi:10.1016/S0960-894X(01)00112-3

Selective δ-opioid receptor ligands: potential PET ligands based on naltrindole

J Clayson
, A R Jales
, R J Tyacke
, A L Hudson
, D J Nutt
, J W Lewis
, S M Husbands

Department of Life Sciences

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

18 Citations (SciVal)

Abstract

Two series of δ-selective ligands related to the prototypic δ-antagonist naltrindole have been prepared and evaluated in opioid binding assays with the aim of developing new PET ligands for the δ-opioid receptor. One compound (5d) had significantly higher selectivity than naltrindole, but with substantially reduced binding affinity. For those compounds retaining similar affinity to naltrindole, those having ethyl and fluoroethyl substituents afforded the highest levels of selectivity. However, none of the compounds combined the high level of affinity and selectivity ideally suited to the development of an imaging agent.

Original language	English
Pages (from-to)	939-943
Number of pages	5
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	11
DOIs	https://doi.org/10.1016/S0960-894X(01)00112-3
Publication status	Published - 2001

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title = "Selective δ-opioid receptor ligands: potential PET ligands based on naltrindole",

abstract = "Two series of δ-selective ligands related to the prototypic δ-antagonist naltrindole have been prepared and evaluated in opioid binding assays with the aim of developing new PET ligands for the δ-opioid receptor. One compound (5d) had significantly higher selectivity than naltrindole, but with substantially reduced binding affinity. For those compounds retaining similar affinity to naltrindole, those having ethyl and fluoroethyl substituents afforded the highest levels of selectivity. However, none of the compounds combined the high level of affinity and selectivity ideally suited to the development of an imaging agent. ",

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T1 - Selective δ-opioid receptor ligands: potential PET ligands based on naltrindole

AU - Clayson, J

AU - Jales, A R

AU - Tyacke, R J

AU - Hudson, A L

AU - Nutt, D J

AU - Lewis, J W

AU - Husbands, S M

PY - 2001

Y1 - 2001

N2 - Two series of δ-selective ligands related to the prototypic δ-antagonist naltrindole have been prepared and evaluated in opioid binding assays with the aim of developing new PET ligands for the δ-opioid receptor. One compound (5d) had significantly higher selectivity than naltrindole, but with substantially reduced binding affinity. For those compounds retaining similar affinity to naltrindole, those having ethyl and fluoroethyl substituents afforded the highest levels of selectivity. However, none of the compounds combined the high level of affinity and selectivity ideally suited to the development of an imaging agent.

AB - Two series of δ-selective ligands related to the prototypic δ-antagonist naltrindole have been prepared and evaluated in opioid binding assays with the aim of developing new PET ligands for the δ-opioid receptor. One compound (5d) had significantly higher selectivity than naltrindole, but with substantially reduced binding affinity. For those compounds retaining similar affinity to naltrindole, those having ethyl and fluoroethyl substituents afforded the highest levels of selectivity. However, none of the compounds combined the high level of affinity and selectivity ideally suited to the development of an imaging agent.

U2 - 10.1016/S0960-894X(01)00112-3

DO - 10.1016/S0960-894X(01)00112-3

M3 - Article

SN - 0960-894X

VL - 11

SP - 939

EP - 943

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

ER -

Selective δ-opioid receptor ligands: potential PET ligands based on naltrindole

Abstract

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