N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) potential delta-opioid receptor PET ligands.

Abstract:

:The properties of two prospective positron emission tomography (PET) ligands for the delta-opioid receptor, N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) were investigated. Both were antagonists in the mouse vas deferens, and showed high affinity and selectivity, 1.81 nM and 3.09 nM respectively. [3H]BU97001 binding to rat whole brain was also of high affinity, K(D) of 0.42 nM of and B(MAX) of 59.95 fmol mg of protein(-1). In autoradiographic studies, it was found to bind to brain areas previously shown to be associated with the delta-opioid receptor and good correlations were found to exist with naltrindole and DPDPE. BU97018 and especially BU97001 appear to show good potential as delta-opioid receptor PET ligands with the incorporation of 18F.

journal_name

Nucl Med Biol

authors

Tyacke RJ,Robinson ES,Schnabel R,Lewis JW,Husbands SM,Nutt DJ,Hudson AL

doi

10.1016/s0969-8051(02)00300-1

keywords:

subject

Has Abstract

pub_date

2002-05-01 00:00:00

pages

455-62

issue

4

eissn

0969-8051

issn

1872-9614

pii

S0969805102003001

journal_volume

29

pub_type

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